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Annotated References

Pages 197-221 | Published online: 03 Mar 2008

Annotated References

  • ABRUZZO GK, FLA1 ihRY AM, GILL CJ, SMITH JG, ICROPPH, BARTIZAL K: Evaluation of water soluble lipopeptides L-733,560, 1,705,589 and L-731,373 in a mouse model of disseminated aspergillosis. Program and Abstracts of the 33rd Interscience Conference on Antimicrobial Agents and Chemotherapy, New Orleans, Louisiana, 1993 Abstr. 355. L-733,560 and L-705,589 but not L-731,373, significantly prolonged survival in a mouse disseminated aspergillosis model at 0.02 mg/kg 43, bid X5.
  • ACTOR P, URI JV, ZAJAC L, GUARINI JR, PHILLIPS L, PITKIN DH, BERGES DA, DUNN GL, HOOVER JRE, WEISBACH J:SKF 75073, a new parenteral broad-spectrum cepha-losporin with high and prolonged serum levels. Antimi-crob. Agents Chemother. (1977) 13:784–790.
  • ADEFARATI AA, HENSENS OD, JONES ETT, TKACZ JS: Pneumocandins from Zalerion arboricola V. Glutamic acid- and leucine-derived amino adds in pneumo-candin Ao (L-671,329) and distinct origins of the substi-tuted proline residues in prieumocandins Ao and Bo. J. Antibiot. (1992) 45:1953–1957.
  • Discusses the distinct biogenesis of the proline residues of pneumo-candin Ao and pneumocandin Bo.
  • ADEFERATI AA, GIACOBBE RA, HENSENS OD, TKACZ JS: Biosynthesis of L-671,329, an echinocandin-type anti-biotic produced by Zalerion arboricola: Origins of some of the unusual amino acids and the di-methylmyristic acid side chain. J. Am. Chem. Soc. (1991) 113:3542–3545.
  • This biosynthetic investigation shows that the 3-hydroxy-4-methyl-proline is derived from leucine not proline. The unusual homotyros-Me is derived from tyrosine and acetate. Lastly, the methyl groups of the side chain come from methionine.
  • ALBORN WEJ, FLOKOWITSCH JE, WU CYE, PRESTON DA, TERNANSKY RJ: Biological evaluation of a series of carbacephems showing broad-spectrum activity in-cluding methicllin-resistant Staphylococcus aureus (MRSA). 33rd Interscience Conference on Antimicrobial Agents and Chemotherapy New Orleans (1993) Abstr. 926.
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  • An important contribution to the evaluation of RP 59500
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  • BALKOVEC JM, BLACK RM: Reduction studies of antifun-gal echinocandin lipopeptides. One step conversion of echinocandin B to echinocandin C. Tetrahedron Lett. (1992) 33:4529–4532.
  • Describes selective reductions at the hemiaminal, and homotyrosine positions of the echinocandin and pneumocandin natural products.
  • BALKOVEC JM, BLACK EM, HAMMOND ML, HECK JV, ZAMBIAS RA, ABRUZZO G, BARTIZAL K, KROPP H, TRAI-NOR C, SCHWARTZ RE, MCFADDEN DC, NOLLSTADT KH, PITTARELLI LA, FOWLES MA, SCHMATZ DM: Synthesis, stability, and biological evaluation of water-soluble prodrugs of a new echinocandin lipopeptide. Discov-ery of a potential clinical agent for the treatment of systemic cadidiasis and Pneumocystis carinii pneumo-nia (PCP). J. Med Chem. (1992) 35:194–198.
  • Prodrugs of pneumocandin Bo (L-688,786) are described. The chemi-cally stable phosphate ester derivative, L-693,989, showed bio-equivalence to the parent compound in rodent models of candidiasis and PCP.
  • BALKOVEC JM, BLACK EM, ABRUZZO GK, BARTIZAL K, DREIKOFtN S, NOLLSTADT K: Pneumocandin antifungal Ilpopeptides. The phenolic hydroxyl is required for 1,3-13-glucan synthesis inhibition. Bioorg. Med. Chem. Lett. (1993) 3:2039–2042.
  • Removal of phenolic hydroxyl of homotyrosine residue of pneumo-candin Bo shows a 140-fold loss in glucan synthesis inhibition.
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  • BARRETT MS, JONES RN, ERWIN ME, JOHNSON DM, BRIGGS BM: Antimicrobial activity evaluations of two new quinolones, PD127391 (CI-960 and AM-1091) and PD131628. Diagn. Microbiol. Infect. Dis. (1991) 14:389–401.
  • BARRETT MS, JONES RN, ERWIN ME, KOONTZ FP: CI-960, sparfloxacin, WIN57273, and isepamicin activity against clinical isolates of Mycobacterium avium-in-tracellularae complex, M. chekmae, and M. fortuitum. Diagn, Micrabiol. Infect. Dis. (1992) 15:169–171.
  • BARR1ERE JC, PARIS JM: RP 59500 and related semisyn-thetic streptogramins. Drugs of the Future (1993), 18(9):833–845. A recent review on RP 59500 and pristinamycins.
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  • BARR1ERE JC, BOUANCHAUD DH, PARIS JM, ROLIN O, HARRIS NV, SMITH C: Antimicrobial activity against Staphylococcus aureus of semi-synthetic injectable steptogramins: RP59500 and related compounds. J. An-timicrob. Chemother. (1992) 30(Suppl A):1–8.
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  • BARRY AL, FUCHS PC, CITRON DM, ALLEN SD, WEXLER HM: Methods for testing the susceptibility of anaerobic bacteria to two fluoroquinolone compounds, PD131628 and clinafloxacin. J. Antimicrob. Chemother. (1993) 31:893–900.
  • BARTIZAL K, ABRUZZO GK, SCHMATZ DM: Biological activity of the pneumocandins. In: Cutaneous Ant fungalAgents (1993). Rippon JW, Fromtling RA (Eds), Marcel Dek-ker, New York. A detailed account of the biological activity of the pneumocandin natural products. Comparisons between these and echinocandins B and C, tetrahydroechinocandins B and C, cilofungin and am-photericin B is made.
  • BARTIZAL K, ABRUZZO G, TRAINOR C, KRUPA D, NOLL-STADT K, SCHMATZ D, SCHWARTZ R, HAMMOND M, BALKOVEC J, VANMIDDLESWORTH F: In vitro antifungal activities and in vivo efficacies of 1,3-13-D-glucan synthe-sis inhibitors L-671,329, L-646,991, tetrahydroechino-candin B, and L-687,781, a papulacandin. Antimicrob. Agents Chemother. (1992) 36:1648–1657.
  • Comparison of pneumocandin Ao, cilofungin and tetrahydroechino-candin B.
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  • BALTERNFEIND A: Comparative in vitro activities of the new quinolone, Bay y 3118, and ciprofioxacin, spar-floxacin, tosufloxacin, CI-960 and CI-990. J. Antimicrob. Chemother. (1993) 31:505–522.
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  • The first account of the echinocandin class of lipopeptides.
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  • BERTHAUD N, MONTAY G, HUET Y, BOURGUES A, BUS- SSIERE JC, SAUTEDE M, SELINGUE M, DESNOTTES JF: RP 59500, in vivo bactericidal activity in a model of S. aureus mouse infection: influence of varying the dos-age and the number of treatments. 32nd International Conference On Antimicrobial Agents And Chemotherapy Anaheim, (1992), Abstr. 1315.
  • BERTHAUD N, ROMBI C, HUET Y, BOURGUES A, BUSSIERE JC, SAUTEDE M, SELINGUE M, DESNO11k,S JF: RP 59500: In vivo bactericidal activity in Streptococcus pneumo-niae mouse septicemia. 33rd International Conference On Antimicrobial Agents And Chemotherapy New Orleans, (1993), Abstr. 1157.
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  • BOUANCHAUD DH: In vitro and in vivo synergic activity and fractional inhibitory concentration (FIC) of the components of a semisynthetic streptogramin, RP 59500.J. Antimicirob. Chem other. (1992) 30(Suppl. A):95-99. A reference article on synergistic activity of streptogramin compo-nents
  • BOUANCHAUD DH: unpublished data.
  • BOUFFARD FA, ZAMBIAS RA, DROPINSKI JF, BALKO'VEC JM, HAMMOND ML, NOLLSTADT KI-1, MARRINAN J: Syn-thesis and antiftmgal activity of water-soluble pneumo-candin Bo derivatives: L-705589, 1,731373, and L–733560.
  • Program and Abstracts of the 33rd Interscience Conference on Antimicrobial Agents and Chemotherapy, New Orleans, Louisiana, 1993 Abstr. 350. Synthesis of pneumocandin analogues L-705,589, L-731,373 and L-733,560 was described. The C. albicans glucan synthase inhibition IC5os were 11, 10 and 1 nM, respectively.
  • BOUFFARD FA, ZAMBIAS RA, DROPINSKI JF, BALKOVEC JM, HAMMOND ML, ABBRUZZO GK, BARTIZAL KF, MAR-RINAN JA, KURTZ MB, MCFADDEN DC, NOLLSTADT RN, POWLES MA, SCHMATZ DM: Synthesis and antifungal activity of novel cationic pneumocandin Bo derivatives. Med. Chem. (1994) 37:(in press). Paper summarizing in vitro and in vivo activity of pneumocandin Bo, L-705,589, L-731,373 and L-733,560.
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  • BRYSKIER A: Une nouvelle amino-2-thiazole cépha-losporine: le céfotiam (SCE 963). Structure, propriétés physicochirniques, bactériologiques et pharmaco-cinétiques. Lyon Pharm (1983) 34:191–203.
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  • Good discussion of factors affecting passive transport of peptides across cellular barriers. Presents a study showing effect of N-methy-lation of peptide bonds on transport across epithelium.
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  • CASEWELL MW, SEYED-AKHAVANI M, WADE J: In vitro activity of RP 59500 against vancomycin-resistant En-terococcus faecium also resistant to 512mg/1 of gen-tamycin. 33rd International Conference On Antimicrobial Agents And Chemotherapy New Orleans,( 1993), Abstr. 1058.
  • CESANA M, BROCCALI G, IMBIMBO BP, CREMA A: Effect of single doses of rufloxacin on the disposition of theophylline and caffeine after single administration. Internl. J. Clin. Pharmacol. Ther. Toxicol. (1991) 29:133–138.
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  • CHAMBERS HF: Studies of RP 59500 in vitro and in a rabbit model of aortic valve endocarditis caused by methicillin-resistant Staphylococcus aureus. J. Antimi-crob. Chemother. (1992) 30 (Suppl. A):117–122.
  • CHANTOT JF, ASZODI J, BONNET A, COSTEROUSSE G, TEUTSCH G: RU 45978 and RU 46069: in vitro and in vivo antibacterial activty of two new broad spectrum No-cephems. 28th Intersci. Conf Antimicrob. Agent Chemother. Los Angeles 1988 Abstr. 436.
  • CHANTOT JF, BRYSKIER A. Cefpirome (HR 810) - Evalu-ation impérimentale de l'activité antibiotique in vitro et in vivo d'une nouvelle amino-2-thi27ole méthoxy-imino céphalosporine. Pathol. Biol. (1985) 33:482–486.
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  • CHIN NX, NEU HC: Post-antibiotic effect of RP 59500 against gram-positive bacteria compared to other agents. 31st International Conference On Antimicrobial Agents And Chemotherapy, Chicago, (1991), Abstr. 899. A relevant article on post-antibiotic effect
  • CHIN NX, HUANG HB, WU JF, NEU HC: In vitro activity of AM-1155, a new fluoroquinolone, compared to other quinolones. 33rd Interscience Conference on Antimicrobial Agents and Chemotherapy, New Orleans, (1993), Abstr. 1007.
  • CHIN NX, HUANG HB, NEU TIC: In vitro activity of DU-6859a, a new fluoroquinolone. 33rd Interscience Con-ference on Antimicrobial Agents and Chemotherapy, New Orleans, (1993), Abstr. 983.
  • CHIN NX, GU JW, NEU HC: In vitro activity of cefcanel versus other oral eephalosporins. Eur. J. Clin. Microbiol. Infect. Dis. (1991) 10:676–682.
  • Good comparison of cephalosporins in vitro.
  • CHIN NX, GU JW, FANG W, NEU HC: In vitro activity of cefquinome, a new cephalosporin, compared with other cephalosporin antibiotics. Diagn. Microbiol. Infect. Dis. (1992) 15:331–337.
  • CHRIST W, LEHNERT T, ULBRICH B: Specific toxicological effects of quinolones. Rev. Infect. Dis. (1988) 10 (Suppl. 1):S141–146,
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  • CLARK AM: The need for new antifungal drugs. In: New Approaches ForAntifungal Drugs(1992). Femandes, BP (Ed), Birkhauser, Boston.
  • COCHEREAU-MASSIN I, et al.: Efficacy and ocular pene- tration of sparfloxacin in experimental streptococcal endophthalmitis. Antimicrob. Agents Chemother. (1993) 37:633–636.
  • COCITO C, CHINALI G: Molecular mechanism of action of virginiamycin-like antibiotics (synergirnycins) on the protein synthesis in bacterial cell-free systems. I Antimicrob. Chemother. (1985) 16(Suppl. A):35-52. A molecular explanation of the synergistic action of virginiamycin antibiotics in vivo is given.
  • COCITO C: Antibiotics of the virginiarnycin family, inhibitors which contain synergistic components. Mi-crobiological Reviews (1979) 43(2):145–198.
  • The reference article on the properties of virginiamycin-like antibi-otics.
  • COCITO C: Properties of virginiamycin-like antibiotics(synergitnycins), inhibitors containing synergisticcomponents In: Antibiotics, Corcoran JN, Hahn FE (Eds), Springer, Berlin, Heidelberg, New York (1983), Vol VI:296–332.
  • An important contribution in reviewing the properties of the strep-togramins.
  • COHEN MA, HUBAND MD, MAILLOUX GB, YODER SL, ROLAND GE, HEIFETZ CL: in vitro activity of sparfloxacin (CI-978, AT-4140, and PD131501) a quinolone with high activity against Gram-positive bacteria. Diagn. Microbiol. Infect. Dis. (1991) 14:403–415.
  • COHEN MA, HUBAND MD, MAILLOUX GB, YODER SL, ROLAND GE, DAMAGALA JM, HEIFETZ CL: In vitro an-tibacterial activities of PD131628, anew 1,8-naphthyrid-ine anti-infective agent. Antimicrob. Agents Chemother. (1991) 35:141–146.
  • COHEN ML: Epidemiology of drug resistance: Implica- ions for a post-antimicrobial era. Science (1992) 257:1050–1055.
  • Discusses the rapid emergence of antibiotic resistance and the concerns for effects on future therapy.
  • COLLATZ E, LABIA R, GUTMANN L: Molecular evolution of ubiquitous beta-lactamases towards extended-spec-trum enzymes against newer beta-lactam antibiotics. Mol. Micro biol. (1990) 4:1615–1620.
  • Excellent reivew of the impact of13-lactamases on cell-wall inhibitors.
  • COLLINS L, MALANOSK1G, WENNERSTEN C, ELIOPOULOS MG, FERRARO MJ, MOELLERING RC:In vitro activity of RP 59500 an injectable streptogramin antibiotic, against vancomycin-resistant gram-positive organisms. 32nd International Conference On Antimicrobial Agents And Che-motherapy Anaheim, (1992), Abstr. 1311.
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  • COOPER MA, ANDREWS JM, WISE R: In vitro activity of PD131628, a new quinolone antimicrobial agent. J. Antimicrob. Chemother. (1992) 29:519–527.
  • COPLEY-MERRIMAN CR, RANSBURG NJ, CRANE LR, KERK-ERING TM, PAPPAS PG, POTTAGE JC, HYSLOP DL: Cilo-fungin treatment of Canditta esopbagitis: Preliminary Phase II results. Program and Abstracts of the 30th Inter-science Conference on Antimicrobial Agents and Chemother-apy, Atlanta, Georgia, 1990 Abstr. 581. Successful treatment of Candida esophagitis in preliminary Phase II studies.
  • COPLEY-MERRIMAN CR, GALLIS H, GRAYBILL JR, DOEB- BELING BN, HYSLOP DL: Cilofungin treatment of dis-seminated cadidiasis: Preliminary Phase 11 results. Pro-gram and Abstracts of the 30th lnterscience Conference on Antimicrobial Agents and Chemotherapy, Atlanta, Georgia, 1990 Abstr. 582. A dose of 500 mg tid was effective for treatment of disseminated candidiasis in Phase II studies with cilofungin.
  • CORSI M, POJANI G, DAL FORNO G, PIETRA C, GAVIRAGHI G, TRIST D: Analysis of the CCICa receptor antagonismof virginiamycin in guinea-pig ileum longitudinal myenteric plexus. Br.J. Pharmacol. (1993) 108:1164–1168.
  • COUROUX P, SCHIEVEN BC, HUSSAIN Z: Pneumocystis carinii. ASM News (1993) 59:179–181.
  • COURTTEU AL, DRUGEON HB, BRYSKIER A, CHUNG SS, REYNAUD AA. Activité comparée de la cefsulodine sur les Pseudomonas aeruginosa, les Actinobacter et les entérobactéries. Pathol. Biol. (1982) 30:432–439.
  • CRAIG W, EBERT S: Pharmacodynamyc activities of RP 59500 in an animal Infection model. 33rd International Conference On Antimicrobial Agents And Chemotherapy, New Orleans, (1993), Abstr. 470.
  • CRUMPLIN GC: Mechanisms of resistance to the 4-qui-• nolone antibacterial agents . Journal of Antimicrobial Che-motherapy (1990) 26(SF):131–144.
  • CULLMANN W: The threat of resistance to the new oral cephalosporins. Chemotherapy (1992) 38:10–17.
  • CURRAN WV, ROSS AA. 70-[2-(2-aminothiazol-4-y1)-(Z)-2- methoxyiminoacetamido]-3[(1,2,3-thiadiazol-5-yfithio methyliceph-3-em-4-carboxylic acid. A new potent cephalosporin derivative. J. Antibiotics (1983) 36:179–180.
  • CURRENT W, BOYLAN CJ, RAAB PA: Anti-Pneumocystis activity of LY303366 and other echinocandin B analogs. Program and Abstracts of the 33rd Interscience Conference on Antimicrobial Agents and Chemotherapy, New Orleans, Louisiana, 1993 Abstr. 368. A 5 mg/kg oral dose of LY303366 gave 99.7% reduction of cysts from the lungs of infected rats in a model of PCP.
  • Rns NAC, EISENSTADT RL, EAST SJ, CORNFORD RJ, WALKER LA, WHITE AJ: Iron-regulated outer membraneproteins of Escbericbia coli K-12 and mechanism of action of catechol-substituted cephalosporins. Antimi-crob. Agents Chemother. (1988) 32:1879–1886.
  • CURTIS NCA, EISENSTADT RI, EAST SJ, CORNFED RJ, WALKER LA, WHITE AJ. Iron-regulated outer membrane proteins of Escbeticbia colt K-12 and mechanism of action of catechol-substituted cephalosporins. Antimi-crob. Agents Chemother. (1988) 32:1879–1886.
  • DABERNAT H, SEGUY, DELMAS C: In vitro activity of RP 59500, a semi-synthetic streptogramin, againstHaemo-pbilus influenzae. 33rd International Conference On Anti timicrobial Agents And Chemotherapy New Orleans, (1993), Abstr. 226.
  • DEBBIA EA, PESCE A, CHIESA M, RICOTTA N, SCFIITO GC: Microbiologk profile of ceftibuten, a new oral cepha-losporin. J. Antibiot. (1992) 18:129–139.
  • DEBONO M, ABBOTT BJ, TURNER JR, HOWARD LC, GOR-DEE RS, HUNT AS, BARNHART M, MOLLOY RM, VUILLARD ICE, FUKUDA D, BUTLER TF, ZECKNER DJ: Synthesis and evaluation of LY121019, a member of a series of semi-synthetic analogues of the antifungal lipopeptide echi-nocandin B. Ann. N.Y. Acad. Sci. (1988) 544:152–167.
  • The full account and structure-activity studies of side chain analogues of echinocandin B by the Lilly group. The choice of cilofungin (LY121019) as a candidate for further study was discussed.
  • DEBONO M, ABBOTT BJ, FUKUDA DS, BARNHART M, WILLARD ICE, MOLLOY RM, MICHEL KR, TURNER JR, BUTLER TF, HUNT AR: Synthesis of new analogs of echinocandin B by enzymatic deacylation and chemical reacylation of the echinocandin B peptide: synthesis of the antifungal agent cilofungin (LY121019). j Antibiot. (1989) 42:389–397.
  • Describes the synthesis and physicochemical properties of cilo-fungin.
  • DEBONO M, TURNER WW, LAGRANDEUR L, BURKHARDT F, RODRIGUEZ M, ZWEIFEL M, NISSEN J, CLINGERMAN K,GORDEE R, ZECKNER D, BUTLER T, PARR T, TANG J: LY303366 - A new semi-synthetic lipopeptide antifungal agent related to echinocandin B. Synthetic and struc-ture-activity studies. Program and Abstracts of the 33rd Interscience Conference on Antimicrobial Agents and Che-motherapy, New Orleans, Louisiana, 1993 Abstr. 359. Poster describing the semi-synthesis and SAR of a number of polyaromatic side chain echinocandin analogues.
  • DEFOSSA E, DÜRCKHEIMER W, FISCHER G, JENDRALLA H, KLESEL N, WOLLMANN T: Cefdaloxime pentexil tosilate (111(916 K) - a diastereomerically pure novel oral cepha-losporinester: synthesis and antibacterial acitivity in vivo. 32nd Interscience Conference on Antimicrobial Agents and Chemotherapy Anaheim (1992) Abstr. 187.
  • DENNING DW, STEVENS DA: Efficacy of cilofungin alone and in combination with amphotericin B in a murine model of disseminated aspergIllosis. Antimicrnb. Agents Chemother. (1991) 35:1329–1333.
  • Cilofungin prolonged survival in this A. fumigatus mouse model at 62.5 mg/kg/day (ip, bid for eleven days) comparable in efficacy to amphotericin B given at 3.3 mg/kg/day (six total doses over eleven days).
  • DESNO1thS JF, DIALLO N: RP 59500: In vitro antistaPhY- lococcal bactericidal activity across platelet-fibrin ma-trices compared to that of vancomycin. 33rd Interna-tional Conference On Antimicrobial Agents And Chemotherapy New Orleans, (1993), Abstact 763.
  • DESNOTTES JF, DIALLO N: Cellular uptake and intracel-lular bactericidal activity of RP 59500 in murine macro-phages. J. Antimicrob. Chemother. (1992) 30(Suppl. A):107–115.
  • DI GAMBATTISTA M, ENGELBORGHS Y, NYSSEN E, CO- CITO C: Kinetics of binding of macrolides, lin-cosamides, and synergimycins to ribosomes. J. Biol. Chem. (1987) 262:8591–8597.
  • DI GAMBATTISTA M, CHINALI G, COCITO C: The molecu-lar basis of the inhibitory activities of the type A and type B synergimycins and related antibiotics on ribo-somes. J. Antimicrob. Chemother. (1989) 24:485–507.
  • DI GAMBATTISTA M, ENGELBORGHS Y, NYSSEN E, CLAYS K, COCITO C: Interaction between virginiamycin S and ribosomes is partly provided by a salt bridge with a Mg2+ Biochemistry (1991) 30:7277-7282. A relevant article on the biological importance of the 3-hydroxy picolinic acid residue in group B streptogramins.
  • DI GAMBATTISTA M, NYSSEN E, PECHER A, COCITO C: Affinity labelling of the virginiamycin S binding site onbacterial ribosome. Biochemistry (1990) 29:9203–9211.
  • An advance in the mechanism of action of streptogramins.
  • DI GAMBATTISTA M, SHARMA NK, ANTEUNIS MJO: Some simple conjugates of virginiamycin and their bio-activ-ity. Bull. Soc. Chim. Beiges (1990) 99:195–211.
  • DOEBBELING BN, FINE BD, PFALLER MA, SHEETZ CT, STOKES TB, WENZEL RP: Acute tubular necrosis (ATN) and anion-gap acidosis during therapy with cilofungin (LY-121019) in polyethylene glycol (PEG). Program and Abstracts of the 30th Interscience Conference on Antimicro-bial Agents and Chemotherapy, Atlanta, Georgia, 1990 Abstr. 583. Toxicity due to PEG-300 cosolvent used in cilofungin formulation.
  • DOOR MB, WEBB CL, BRON N, JASSOS AB: Single-dose tolerance and pharmacokinetics of CI-960 (P1)127391) In healthy volunteers. 31st Interscience Conference of Antimicrobial Agents and Chemotherapy, Chicago, (1991), Abstr. 1154.
  • DUBOIS J, JOLY JR: In vitro activity of RP 59500, a new synergistic antibacterial agent, against Legionella spp. Antimicrob. Chemother. (1992) 30(Suppl. A):77–82.
  • DeRCICHEIMER W, BLUMBACH J, LATRELL R, SCHEUNE-MANN RH Recent development in the field of O-1actam antibiotics. Ang Chem (1985) 24:180–202.
  • EJIMA A, HAYANO T, EBATA T, NAGAHARA T, KODA H, TAGAWA H, FURUKAWA M. Synthesis and antimicrobial activity of cephalosporins with a 1-pyridinium substi-tuent carrying a 5-membered heterocycle at the C-3 position. J. Antibiotics (1987) 40:43–48.
  • EL SOLH N, LONCLE V, AUBERT S, CASETTA A, ALLIGNET J: Analysis of Staphylococcal elements conferring resis-tance to streptogramin A (RP 54476). 33rd International Conference On Antimicrobial Agents And Chemotherapy New Orleans, (1993), Abstr. 217.
  • ELIOPOULOS GM, KLIMM K, ELIOPOULOS CT, FERRARA MJ, MOELLERING RC:In vitro activity of CP-99,219, a new fluoroquinolone, against clinical isolates of Gram-posi-tive bacteria. Antimicrob. Agents Chemother. (1993) 37:366–370.
  • ENG RHK, CHERUBIN C, SMITH SM, BUCCINI F: Inoculum effect of 13-lactam antibiotics on Enterobacteriaceae. Antimicrob. Agent Chemother. (1985) 28:601–606.
  • ENGLISH AR, RETSEMA JA, GIRARD AE, LYNCH JE, BARTH WE: CP-45,899, a beta-lactamase inhibitor that extends the antibacterial spectrum of beta-lactatns: initial bac-teriological characterization. Antimicrobial Agents and Chemotherapy (1978) 14:414–419.
  • ETIENNE SD, MONTAY G, LE LIBOUX A, FRYDMAN A, GARAUD JJ: A phase I, double-blind, placebo-controlled study of the tolerance and pharmacokinetic behaviour of RP 59500. J. Antimicrob. Chemother. (1992) 30(Suppl. A):123–131.
  • The first study published on tolerance and pharmacokinetics of RP 59500 in man.
  • EVANS DA, WEBER AE: Synthesis of the cyclic hexapep- tide echinocandin D. New approaches to the asymmet-ric synthesis of 13-hydroxy a-amino acids. J. Am. Chem. Soc. (1987) 109:7151–7157.
  • Second synthesis of echinocandin D.
  • FANTIN B., VALLOIS DM., OTTAVIANI M, MAZIERE B, GARRY L, POCIDALO JJ, CARBON C: Autoradiographic Pattern of diffusion of "C RP 59500 throughout infected cardiac vegetation in rabbits. 33rd International Confer-ence On Antimicrobial Agents And Chemotherapy New Or-leans, (1993), Abstr. 161.
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  • FELMINGHAM D, ROBBINS MJ, GHOSH G, et al.: In vitro studies with DU-6859a, a new fluoroquinolone antimi-crobiaL 33rd Interscience Conference on Antimicrobial Agents Chemotherapy, New Orleans, (1993), Abstr. 981.
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  • FIRESTONES RA, FAHEY JL, MACIEJEWICZ NS, PATEL GS, CHRISTENSEN BG: Total synthesis of (±)-1-carbacefoxi-tin and cefamandole and (±)-1-oxacefamandole. J. Med. Chem. (1977) 20:551–556.
  • FONT DE MORA J, HERRERO E, SENTANDREU R: A kinetic study on the regeneration of Candida albicans proto-plasts in the presence of cell wall synthesis inhibitors. FEMS Microbiot Lett. (1993) 108:43–48.
  • Study shows that glucans are still formed in the presence of 13-(1,3)-glucan synthesis inhibitors, but the glucan is no longer cell wall bound. FOORD RD: Cefuroxime: human pharmacokinetics. An-timicrob. Agents Chemother. (1976) 9:741–750.
  • FORD AS, BALTCH AL, SMITH RP, RITZ W: In vitro suscep-tibilities of Pseudomonas aeruginosa and Pseudo-monas spp. to the new fluoroquinolones clinafloxacin and P13131628 and nine other antimicrobial agents. J. Antimicrob. Chemother. (1993) 31:523–532.
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  • FOURTILLAN JB, LEROY A, LEFEBVRE MA, HUMBERT G, FILLASTRE JP, REUMONT G, RAMIS N: Cross-over study of pharmacokinetics of cefonicid administered intrave-nously or intramuscularly to healthy adult humans. Eur. J. Drug Metab. Pharrnacok. (1985) 10:225–230.
  • FOURTILLANp, BRISSON AM, BECQ-GIRAUDON B: Etude pharmacocinétique de la cefopérazone (T-1551) chez l'honune, aprés administration intraveineuse de doses de 1 gramme et 2 grammes. Dosages effectués par chromatographie liquide haute performance. Med. Mal. Infect. (1982) 12 (Suppl):21–26.
  • FOURTILLAN JB, BRYSKIER A, MIGNOT A, BORSA F, HUM-BERT G: Pharmacokinetic study of cefmenoxime (SCE-1365-CMX) in healthy adults. Am . J. Med. (1984) 77 (Suppl. 6A):28–31.
  • FOURTILLAN JB, BRISSON AM: Pharmacocinétique com-parée du moxalactam et d'autres céphalosporines. Se-maines des Hopitaux de Paris (1983) 59:1968–1971.
  • FOX R, NEAL KR, LEEN CLS, ELLIS ME, MANDAL BK: Fluconazole resistant Candida in AIDS. J. Infect. (1991) 22:201–204.
  • FRANKMOLLE WP, LARSEN LK, CAPLAN FR, PATTERSON GML, KNUBEL G, LEVINE IA, MOORE RE: Antifungal cyclic peptides from the terrestrial blue-green algaAnabaena-taxa .1. Isolation and biological properties. J. Antibiot. (1992) 45:1451–1457.
  • FRANKMOLLE WP, KNUBEL G, MOORE RE, PAI1ERSONGML: Antifungal cyclic peptides from the terrestrial blue-green alga Anabaena-laxa .2. Structures of laxaphycins A, B, D and E. J. Antibiot. (1992) 45:1458–1466.
  • FRANZBLAU SG, PARRILLA MLR, CHAN GP: Sparfloxacin is more bactericidal than ofloxacin against Mycobac-terium leprae in mice. Intl. J. Lepro. (1993) 61:66–69.
  • FREMALTX A, SISSIA G, COHEN R, GESLIN P: In vitro activity of RP 59500, a new semisynthetic strepto-gramin, against Streptococcus pneumoniae. J. Antimi-crob. Chemother. (1992) 30 (Suppl. A):19–24.
  • FREMAUX A, SISSIA G, ROSEMBAUM M, GESLIN P: In vitro activity of cefpirome (HR 810), anew parenteral cepha-losporin against penicillin susceptible and resistant pneumococci 32nd Intersci. Conf. Antimicrob. Agent Chemother. Anaheim 1992. Abstr. 1020.
  • FROMTLING RA, ABRUZZO GK: L-671,329, a new antifun- gal agent. M. In vitro activity, toxicity, and efficacy in comparison to aculeacin. J. Antibiot. (1989) 42:174-178. A direct comparison in vitro and in vivo of pneumocandin Ao (L:671,329) and aculeacin. The compounds possess similar poten-cies.
  • FROST DJ, DRAKE RR, WASSERMAN BP: (1,3)-13-Glucan synthase from Saccharomyces cerevisiae . In vitro acti-vation by O-lactoglobulin or Brij-35, and photoaffinhy labeling of enriched microsomal fractions with 5-azido-UDP-Glc and 8-azido-GTP. Curr. Microbiol. (1992) 24:295–300.
  • FU KP, LAFREDO SC, FOLENO B, ISAACSON DM, BARRETT JF, TOBIA AJ, ROSENTHALE, ME: In vitro and in vivoantibacterial activities of levofloxacin (1-ofloxacin), an optically active ofloxacin. Antimicrob. Agents Chemother. (1992) 36:860–866.
  • FU K.P, FOLENO BD, LAFREDO SC, LOCOCO JM, ISAACSON DM:In vitro and in vivo antibacterial activities of FK037, a novel parenteral broad-spectrum cephalosporin. An-timicrob. Agents Chemother. (1993) 37:301–307.
  • FUCHS PC, BARRY AL, PFALLER MA, ALLEN SD, GERLACH EH: Multicenter evaluation of the in vitro and in vivo activities of three new quinolones, sparfloxacin, CI-960 and PD131628, compared with the activity of ciproflox-acin against 5,252 clinkal bacterial isolates. Antimicrob. Agents Chemother. (1991) 35:764–766.
  • FUJIE R, YOSHIOKA H, OKUNO A, FUJITA K, MURONO K, SAKATA SMH, ISEKI K, WAGATSUMA Y et al.: Pharnaacok-inetic and clinical studies of cefditoren pivoxil in the pediatric field. Jpn. J. Antibiot. (1993) 46:95–114.
  • FUJII R, NISHIMURA T, SUNAKAWA K: Cefditoren pivoxil (CDTR-PI): pharmacokinetics. Influence on carnitine metabolism and clinical evaluation in pediatric pa-tients. 33rd Interscience Conference on Antimicrobial Agents and Chemotherapy New Orleans (1993) Abstr. 897.
  • FUJII R, SUNAKAWA K, YAMAMOTO S: Carnitine status of S-1108 in pediatric patients with various infectious diseases. 32nd Interscience Conference on Antimicrobial Agents and Chemotherapy Anaheim (1992) Abstr. 186.
  • FUKASAWA M, NOGUCHI H, OKUDA T et al.: In vitro antibacterial activity of SM-1652, a new broad spectrum cephalosporin with antipseudomonal activity. Antimi-crob. Agents Chemother. (1983) 23:195–200.
  • FUKUOKA Y, IKEDA Y, YAMASHIRO Y, TAKAHATA M, TODO Y, NARITA H: In vitro and in vivo antibacterial activities of T-3761, a new quinolone derivative. Antimi-crob. Agents Chemother. (1993) 37:384–392.
  • GALLIS HA, DREW RH, PICKARD WW: Amphotericin B: 30 years of clinical experience. Rev. Infect. Dis. (1990) 12:308–329.
  • GARCIA I, PASCUAL A, GUZMAN MC, PEREA EJ: Uptake and intracellular activity of sparfloxacin in human polymorphonuclear leukocytes and tissue culture cells. Antimicrob. Agents Chemother. (1992) 36:1053–1056.
  • GEM F RT M, MIZUUCHI K, O'DEA MH, ITOH T, TOMIZAWA J: Nalidixic acid resistance: a second genetic charac-teristic involved in DNA gyrase activity. Proceedings of the National Academy of Science, USA (1977) 74:4772–4776.
  • GEORGOPAPADAKOU NH, ALBRECHT HA, BERTASSO A, MCCAFFREY C: Mode of action of Ro 25–0534, a 3'-tertiary amine-linked dual action cephalosporin. 33rd Inter-science Conference on Antimicrobial Agents and Chemother-apy New Orleans (1993) Abstr. 1493.
  • GEORGOPOULOS A, BREYER S, FEISTANER S, STAUFFER F, MARKRISTATH1S A, GEORGOPOULOS M., GRANINGER W: Bactericidal effect of RP 59500 against staphylococci with different phenotypes in a diffusion chamber model in rabbits. 32nd International Conference On An-timicrobial Agents And Chemotherapy Anaheim, (1992), Abstr. 1309.
  • GIBBONS A: Exploring new strategies to fight drug-re-sistant microbes. Science (1992) 257:1036–1038.
  • Gives an editorial overview of the implications of antibiotic resis-tance.
  • GILFILLAN EC, PELAK AB, FROMTLING RA, BLAND J, HADLEY S, GADEBUSH HH: L-656575 (0PC-9-176): a novel oxacephem. Pharmacokinetics and experimental Chemotherapy. J. Antibiotics (1988) 41:1137–1141.
  • GIRARD AE, FAIELLA JA, CIMOCHOWSKI CR, BRIGHTY KE: In vivo activity of CP-99,219 in models of acute and localized infection in mice. 33rd Interscience Conference on Antimicrobial Agents and Chemotherapy, New Orleans, (1993), Abstr. 1510.
  • GLADUE RP, BRIGHT GM, ISAACSON RE, NEWBORG MF: In vitro and in vivo uptake of azhhromycin (CP-62,993) by phagocytic cells: possible mertmoism of delivery and release at sites of infection. Antimicrobial Agents and Chemotherapy (1989) 33:277–282.
  • Describes a novel method of drug delivery to sites of infections.
  • GOHARA Y, et al.: In vitro and in vivo activities of Q-35, a new fluoroquinolone, against Mycoplasma pneumo-niae. Antimicrob. Agents Chemother. (1993) 37:1826–1830.
  • GOLDSTEIN EJ: Patterns of susceptibility to fluoroqui-nolones among anaerobic bacterial isolates in the United States. Clin. Infect. Dis. (1993) 16 (Suppl. 4):S377–S381.
  • GOLDSTEIN EJC, CITRON DM: Comparative activity of ciprofloxacin, ofloxacin, sparfloxacin, temafloxacin, CI-960, CI-990, and WIN 57273 against anaerobic bac- teria. Antimicrob. Agents Chemother. (1992) 36:1158-1162. A thorough data summary describing the in vitro activity of several quinolones against clinically important anaerobes.
  • GOLLAPUDI SV, CHUAH SK, HARVEY T, THADEPALLI FID, TFIADEPALLI H: In vivo effects of rufloxacin and ciprofloxacin on T-cell subsets and tumor necrosis factor production in mice infected with I3acteroides fragilis. Antimicrob. Agents Chemother. (1993) 37:1711–1712.
  • GOODING BB, JONES RN:In vitro antimicrobial activity of CP-99,219, a novel azabicyclo-naphthyridone. An-timicrob. Agents Chemother. (1993) 37:349–353.
  • GOOTZ TD, BRIGHTY ICE, ANDERSON ME, HASKELL SL, SUTCLIFFE JA, CASTALDI MJ, MILLPR SA: In vitro activity and synthesis of CP-99,219, a novel 7-(3-azabicy-clo[3.1.0] hexyDnaphthyridone. 32nd Interscience Con-ference on Antimicrobial Agents and Chemotherapy, Ana-heim, (1992), Abstr. 751.
  • GORDEE R, FARMER J, FLOKOWITSCH J, HAEBER P: In vitro antifungal activity of LY303366, a new antifungal agent derived from echinocandin B. Program and Ab-stracts of the 33rd Interscience Conference on Antimicrobial Agents and Chemotherapy, New Orleans, Louisiana, 1993Ab-stract 360. Poster presenting the activity of LY303208, LY303366 and LY307863 against Candida, Aspergillus, Blastomyces, Histoplasma and Crypto-coccus. Kill curves demonstrate the fungicidal nature of LY303366.
  • GORDEE R, FARMER J, ZECKNER D: LT295337 a novel cyclic depsipeptide antifungal antibiotic. L In vitroantifungal activity. Program and Abstracts of the 32nd Interscience Conference on Antimicrobial Agents and Che-motherapy, Anaheim, California, 1992, Abstr. 496.
  • GORDEE RS, ZECKNER DJ, ELLIS LF, THAKKAR AL, HOWARD LC: In vitro and in vivo anti-Candida activity and toxicology of LY121019. J. Antibiot. (1984) 37:1054–1065.
  • Contains a full description of activity, and toxicology results with cilofungin and several side chain analogues.
  • GORDEE RS, ZECKNER DJ, HOWARD LC, AIBORN WE, DEBONO M: Anti-Candida activity and toxicology of LY121019, a novel semisynthetic polypeptkle antifun- gal antibiotic. Ann. N.Y. Acad. Sci. (1988) 544:294–301.
  • The activity and toxicity of cilofungin is presented.
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  • Aculeacin A acylase is apparently the same enzyme described by Lilly for the deacylation of echinocandin B.
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  • Describes the structure determination, and crystal structure of echi-nocandin B and several heavy-atom derivatives.
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  • Good comparison of different susceptibilities to I3-lactamases.
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  • KORTEN U, TOMAYKO JF, MURRAY BE: DU-6859a, a new fluoroquinolone agent: comparative in vitro activity against Gram-positive cocci. 33rd Interscience Conference on Antimicrobial Agents and Chemotherapy, New Orleans, (1993), Abstr. 985.
  • KOSUGE K, WADA K, et al.: Phase I study of AM-1155. 32nd Interscience Conference on Antimicrobial Agents and Chemotherapy, Anaheim, (1992), Abstr. 1003.
  • KOUPAL LR, WEISSBERGER B, SHUNGU DL, WEINBERG E, GRADEBUSH H: Quarternary heterocyclylamino tams . II. The in vitro antibacterial properties of L 640876 a new type of f3-lactam antibiotic. J. Antibiotics (1983) 36:47–53.
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  • First total synthesis of an echinocandin natural product.
  • KUROKAWA N, OHFUNE Y: Synthetic studies on antifun-gal cyclic peptides, echinocandins - Stereoselective total synthesis of echinocandin D via a novel peptide cou-pling. Tetrahedron (1993) 49:6195–6222.
  • Full account of the JACS communication. Attempts to prepare echinocandin B were unsuccessful.
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  • LABRO MT, BRYSKIER A: imrnunomodulating properties of new cephalosporins: a preliminary cLIssificallon. Chimiotherapia (1987) 6 (Suppl 2):219–221.
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  • LALANDE V, et al.: Powerful bactericidal activity of spar-floxacin against Mycobacterium tuberculosis in mice. Anttmicrob. Agents Chemother. (1993) 37:407–413.
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  • LEWIN C, DOHERTY C, GOVAN J: In vitro activities of meropenem, PD127391, PD131628, ceftazidime, chlora.mphenicol, co-trimaxazole, and ciprofloxacin against Pseudomonas cepacia. Antimicrob. Agents Chemother. (1993) 31:123–125.
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  • LIMBERT M, ISERT D, KLESEL N, MARKUS A, SEEGER K, SEIBERT G, SCHRINNER E: Antibacterial activities in vitro and in vivo and pharmacokinetics of cefquinome (HR 111V), a new broad-spectrum cephalosporin. Antimi-crob. Agents Chemother. (1991) 35:14–19.
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  • An excellent review of current antifungal agents useful for systemic infection and of experimental agents in development. The review covers the polyenes, flucytosine, azoles and other investigational compounds.
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  • First pneumocandin to be isolated.
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