Pharmacological significance of triazole scaffold

References

• Holla BS, Mahalinga M, Karthikeyen MS, Poojary B, Akberali PM, Kumari NS. Synthesis, characterization and antimicrobial activity of some substituted 1,2,3-triazoles. Eur J Med Chem 2005;40:1173–1178.
   PubMed Web of Science ®Google Scholar
• Sanghvi YS, Bhattacharya BK, Kini GD, Matsumoyo SS, Larson SB, Jolley WB, Robins RK, Revankar GR. Growth inhibition and induction of cellular differentiation of human myeloid leukemia cells in culture by carbamoyl congeners of ribavirin. J Med Chem 1990;33:336–344.
   PubMedGoogle Scholar
• Chen MD, Lu SJ, Yuag GP, Yang SY, Du XL. Synthesis and antimicrobial activity of some heterocyclic beta-enamino ester derivatives with 1,2,3-triazole. Heterocyclic Comm 2000;6:421–426.
   Web of Science ®Google Scholar
• Sherement EA, Tomanov RI, Trukhin EV, Berestovitskaya VM. Synthesis of 4-aryl-5-nitro-1,2,3-triazoles. Russ J Org Chem 2004;40:594–595.
   Google Scholar
• Hafez HN, Abbas HA, El-Gazzar AR. Synthesis and evaluation of analgesic, anti-inflammatory and ulcerogenic activities of some triazolo- and 2-pyrazolyl-pyrido[2,3-d]-pyrimidines. Acta Pharm 2008;58:359–378.
   PubMed Web of Science ®Google Scholar
• Banu KM, Dinaker A, Ananthnarayan C. Synthesis, characterization of antimicrobial studies and pharmacological screening of some substituted 1,2,3-triazoles. Indian J Pharm Sci 1999;61:202–205.
   Google Scholar
• Guan LP, Jin QH, Tian GR, Chai KY, Quan ZS. Synthesis of some quinoline-2(1H)-one and 1,2,4-triazolo [4,3-a]quinoline derivatives as potent anticonvulsants. J Pharm Sci 2007;10:254–262.
   Web of Science ®Google Scholar
• Passannanti A, Diana P, Barraja P, Mingooia F, Lauria A, Cirrincine G. Pyrrolo[2,3-d][1,2,3]triazoles as potential antineoplastic agents. Heterocycles 1998;48:1229–1235.
   Web of Science ®Google Scholar
• Gujjar R, Marwaha A, White J, White L, Creason S, Shackleford DM, Baldwin J, Charman WN, Buckner FS, Charman S, Rathod PK, Phillips MA. Identification of a metabolically stable triazolopyrimidine-based dihydroorotate dehydrogenase inhibitor with antimalarial activity in mice. J Med Chem 2009;52:1864–1872.
   PubMed Web of Science ®Google Scholar
• Johns BA, Weatherhead JG, Allen SH, Thompson JB, Garvey EP, Foster SA. The use of oxadiazole and triazole substituted naphthyridines as HIV-1 integrase inhibitors Part 1: Establishing the pharmacophore. Bioorg Med Chem Lett 2009;19:1802–1806.
   PubMed Web of Science ®Google Scholar
• Manfredini S, Vicentini CB, Manfrini M, Bianchi N, Rustigliano C, Mischiati C, Gambari R. Pyrazolo-triazoles as light DNA cleaving agents. Bioorg Med Chem 2000;8:2343–2346.
   PubMed Web of Science ®Google Scholar
• Duran A, Dogan HN, Rollas H. Synthesis and preliminary anticancer activity of new 1,4-Dihydro-3-(3-hydroxy-2-naphthyl)-4-substituted-5H-1,2,4-triazoline-5-thiones. Farmaco 2002;57:559–564.
   PubMedGoogle Scholar
• Sztanke K, Tuzimski T, Rzymowska J. Synthesis, determination of the lipophilicity, anticancer and antimicrobial properties of some fused 1,2,4-triazole derivatives. Eur J Med Chem 2008;43:404–419.
   PubMed Web of Science ®Google Scholar
• Gilchrist TL. Heterocyclic Chemistry. Singapore: Pearson Education India, 2005:298–307.
   Google Scholar
• Liu P, Zhu S, Xie W. Synthesis and SAR studies of biaryloxy-substituted triazoles as antifungal agents. Bioorg Med Chem Lett 2008;18:3261–3265.
   PubMed Web of Science ®Google Scholar
• Holmes CB, Losina E, Walensky RP. Review of human immunodeficiency virus type I-related opportunistic infections in sub-Saharan Africa. Clin Infect Dis 2003;36:652–662.
   PubMed Web of Science ®Google Scholar
• Brumfitt W, Hamilton-Muller JMT. The challenges of methicillin-resistant Staphylococcus aureus. J Drug Exp Clin Res 1994;20:215–224.
   PubMedGoogle Scholar
• Neu HC. The crisis in the antibiotic resistance. Science 1992;257:1064–1074.
   PubMed Web of Science ®Google Scholar
• Vicini P, Geronikaki A, Anastasia K, Incerti M Zani F. Synthesis and antimicrobial activity of novel 2-thiazolylimino-5-arylidene-4-thiazolidinones. Bioorg Med Chem 2006;14:3859–3864.
   PubMed Web of Science ®Google Scholar
• Fridkin SK, Jarvis WR. Epidemiology of nosocomial fungal infections. Clin Microbiol Rev 1996;94:499–511.
   Google Scholar
• Sheehan DJ, Hitchcock CA, Sibley CM. Current and emerging azole antifungal agents. Clin Microbiol Rev 1999;12:40–79.
   PubMed Web of Science ®Google Scholar
• Demir-Erol D, Calis U, Demirdamar R, Nulug N, Ertan M. Synthesis and biological activities of some 3,6-disubstituted-thiazolo[3,2-b][1,2,4]triazoles. J Pharm Sci 1995;84:462–465.
   PubMedGoogle Scholar
• Jana C, Julius S. Resistance in fluconazole-resistant Candida albicans, isolates from vaginal candidiasis. Int J Antimicrob Agents 2006;27:403–408.
   PubMedGoogle Scholar
• Kaufmann C, Hedderwick SA. Treatment of systemic fungal infections in older patients: achieving optimal outcomes. Drugs Aging 2001;18:313–324.
   PubMedGoogle Scholar
• Linnbur SA, Parnes BL. Pulmonary and hepatic toxicity due to nitrofurantoin and fluconazole treatment. Ann Pharmacother 2004;38:612–616.
   PubMedGoogle Scholar
• Sheng C, Zhang W, Ji H, Zhang M, Song Y, Xu H, Zhu J, Miao Z, Jiang Q, Zhou Y, Zhu J, Lu J. Structure based optimization of azole antifungal agents by CoMFA, CoMSIA, and molecular docking. J Med Chem 2006;49:2512–2525.
   PubMed Web of Science ®Google Scholar
• Boyle FT, Gilman DJ, Gravestock MB, Wardleworth JM. Synthesis and structure activity relationships of a novel antifungal agent ICI 195739. Ann NY Acad Sci 1988;544:86–100.
   PubMedGoogle Scholar
• Parke JS, Yu KA, Kang TH, Kim S, Toung-Gersuh YG. Discovery of novel imidazole-linked triazoles as antifungal agents. Bioorg Med Chem Lett 2007;17:3486–3490.
   PubMedGoogle Scholar
• Lebouvier N, Pegniez F, Duflos M, Borgne LE. Synthesis and antifungal activities of new fluconazole analogues with azaheterocycle moiety. Bioorg Med Chem Lett 2007;17:3686–3689.
   PubMed Web of Science ®Google Scholar
• Demirayak S., Benkli K., Guven K. Synthesis and antimicrobial activities of some 3-arylamino-5-[2-(substituted imidazole-1-yl or benzimidazol-1-yl)ethyl]-1,2,4-triazole derivatives. Eur J Med Chem 2000;35:1037–1040.
   PubMed Web of Science ®Google Scholar
• Gill C, Jadhav G, Shaikh M, Kale R. Clubbed [1,2,3] triazoles by fluorine benzimidazole: a novel approach to H37Rv inhibitors as a potential treatment for tuberculosis. Bioorg Med Chem Lett 2008;18:6244–6247.
   PubMed Web of Science ®Google Scholar
• Zitouni GT, Chevallet P, Kaya D. Synthesis and antimicrobial activity of 4-phenyl/cyclohexyl-5-(1-phenoxyethyl)-3-[N-(2-thiazolyl)acetamido]thio-4H-1,2,4-triazole derivatives. Eur J Med Chem 2005;40:607–613.
   PubMed Web of Science ®Google Scholar
• Pokrovskaya V, Belakhov V, Hainrichson M, Yaron S, Baasov T. Design, synthesis, and evaluation of novel fluoroquinolone-aminoglycoside hybrid antibiotics. J Med Chem 2009;52:2243–2254.
   PubMed Web of Science ®Google Scholar
• Pintilie O, Profire L, Sunel V, Popa M, Pui A. Synthesis and antimicrobial activity of some new 1,3,4-thiadiazole and 1,2,4-triazole compounds having a D,L-methionine moiety. Molecules, 2007;12:103–113.
   PubMed Web of Science ®Google Scholar
• Holla BS, Rao BS, Sarojini BK, Akberali PM, Kumari NS. Synthesis and studies of some new fluorine containing triazolothiadiazines as possible antibacterial, antifungal and anticancer agents. Eur J Med Chem 2006;41:657–663.
   PubMed Web of Science ®Google Scholar
• Sangshetti JN, Nagawade RR, Shinde DB. Synthesis of novel 3-(1-(1-substituted piperidin-4-yl)-1H-1,2,3-triazol-4-yl)-1,2,4-oxadiazol-5(4H)-one as antifungal agents. Bioorg Med Chem Lett. 2009;19:3564–3567.
   PubMed Web of Science ®Google Scholar
• Isloor AM, Kalluraya B, Shetty P. Regioselective reaction: synthesis, characterization and pharmacological studies of some new Mannich bases derived from 1,2,4-triazoles. Eur J Med Chem 2009;44:3784–3787.
   PubMed Web of Science ®Google Scholar
• Xie W, Chipman DL, Robertson RL, Erikson DL. Expression of mitogen-responsive gene encoding prostaglandin synthase is regulated by mRNA splicing. Proc Natl Acad Sci USA 1991;88:2692–2696.
   PubMed Web of Science ®Google Scholar
• Kajubu DA, Fletcher BS, Varnum BC, Lim RW, Herschman HR. Regulation of COX-2 expression in human cancers. J Biol Chem 1991;266:12866–12872.
   PubMedGoogle Scholar
• Hinz B, Brune KJ. cyclooxygenase-2: 10 years later. J Pharm Exp Ther 2002;300:367–375.
   PubMed Web of Science ®Google Scholar
• DeWitt DL. COX-2 selective inhibitors: new super aspirins. Mol Pharmacol 1999;55:625–631.
   PubMed Web of Science ®Google Scholar
• Mitchell JA, Akarasereenont C, Thiemermann RJ, Flower JR, Vane JR. Selectivity of nonsteroidal anti-inflammatory drugs as inhibitors of constitutive and inducible cyclooxygenase. Proc Natl Acad Sci USA 1993;90:11693–11697.
   PubMed Web of Science ®Google Scholar
• Tozkoparan B, Kupeli E, Yesilada E, Ertan M. Preparation of 5-aryl-3-alkylthio-l,2,4 triazoles and corresponding sulfones with antiinflammatory-analgesic activity. Bioorg Med Chem 2007;15:1808–1814.
   PubMed Web of Science ®Google Scholar
• Kumar H, Javed SA, Khan SA. 1,3,4-Oxadiazole/thiadiazole and 1,2,4-triazole derivatives of biphenyl-4-yloxy acetic acid: synthesis and preliminary evaluation of biological properties. Eur J Med Chem 2008;43:2688–2698.
   PubMed Web of Science ®Google Scholar
• Mohamed BG, Abdel-Alim AA, Hussein MA. Synthesis of 1-acyl-2-alkylthio-1,2,4-triazolobenzimidazoles with antifungal, anti-inflammatory and analgesic effects. Acta Pharm 2006;56:31–48.
   PubMedGoogle Scholar
• Abdel-Rahman HM, Hussein MA. Synthesis of beta-hydroxypropanoic acid derivatives as potential anti-inflammatory, analgesic and antimicrobial agents. Arch Pharm 2006;339:378–387.
   PubMed Web of Science ®Google Scholar
• Wuest F, Tang X, Kniess T, Pietzsch J, Suresh M. Synthesis and cyclooxygenase inhibition of various (aryl-1,2,3-triazole-1-yl)-methanesulfonylphenyl derivatives. Bioorg Med Chem 2009;17:1146–1151.
   PubMed Web of Science ®Google Scholar
• Moise M, Sunel V, Profire L, Popa M, Desbrieres J, Peptu C. Synthesis and biological activity of some new 1,3,4-thiadiazole and 1,2,4-triazole compounds containing a phenylalanine moiety. Molecules 2009;14:2621–2631.
   PubMed Web of Science ®Google Scholar
• UK Cancer Incidence Statistics by Age. Cancer Research UK. 2007:6–25.
   Google Scholar
• Cancer. World Health Organization. Feb, 2006:6–25.
   Google Scholar
• Report sees 7.6 Million Global 2007 Cancer Deaths. American Cancer Society. December, 2007.
   Google Scholar
• Edwards P J. Thiazolidinone derivatives targeting drug-resistant lung cancer cells. Drug Discovery Today 2008;13:1107–1108.
   Google Scholar
• Zhai X, Zhao YF, Liu YJ, Zhang Y, Xun FQ, Liu J, Gong P. Synthesis and cytotoxicity studies of novel [1,2,4]triazolo[1,5-a]pyrimidine-7-amines. Chem Pharm Bull 2008;56:941–945.
   PubMedGoogle Scholar
• McArthur HL, Gelmon KA, Olivotto IA, Speers CH, Ellard SL, O′Reilly SE, Kennecke HF. Effectiveness of a letter notification program for women with early-stage breast cancer eligible for extended adjuvant letrozole. J Clin Oncol 2009;27:1388–1393.
   PubMedGoogle Scholar
• Ibrahim DA. Synthesis and biological evaluation of 3,6-disubstituted[1,2,4]triazolo[3,4-b][1,3,4]thiadiazole derivatives as a novel class of potential anti tumor agents. Eur J Med Chem 2009;44:2776–2781.
   PubMed Web of Science ®Google Scholar
• Lin R, Connolly PJ, Huang S. 1-Acyl-1H-[1,2,4]triazole-3,5-diamine analogues as novel and potent anticancer cyclin dependent kinase inhibitors: synthesis and evaluation of biological activities. J Med Chem 2005;48:4208–4211.
   PubMed Web of Science ®Google Scholar
• El-Hawash SA, Habib NS, Kassem MA. Synthesis of some new quinoxalines for evaluation of in vitro antitumor and antimicrobial activities. Arch Pharm 2006;339:564–571.
   PubMed Web of Science ®Google Scholar
• Zhang Q, Pan J, Zheng RL, Wang Q. Redifferentiation of human hepatoma cell induced by 6-(p-chlorophenyl)-3-[1-(p-chlorophenyl)-5-methyl-1H-1,2,3-triazol-4-yl]-s-triazolo[3,4-b]-1,3,4-thiadiazole(TDZ). Pharmazie 2005;60:378–382.
   PubMed Web of Science ®Google Scholar
• Pachuta-Stec A, Rzymowska J, Mazur L, Mendyk E, Pitucha M, Rzaczyńska Z. Synthesis, structure elucidation and antitumour activity of N-substituted amides of 3-(3-ethylthio-1,2,4-triazol-5-yl)propenoic acid. Eur J Med Chem 2009;44:3788–3793.
   PubMed Web of Science ®Google Scholar
• Haslam DW, James WP. Obesity. Lancet 2005;366:1197–1209.
   PubMed Web of Science ®Google Scholar
• Poulsen SA, Wilkinson BL, Innocenti A. Inhibition of human mitochondrial carbonic anhydrases VA and VB with para-(4-phenyltriazole-1-yl)-benzene sulphonamide derivatives. Bioorg Med Chem Lett 2008;18:4624–4627.
   PubMed Web of Science ®Google Scholar
• Tierney LM, McPhee SJ, Papadakis MA. Current Medical Diagnosis and Treatment. New York: Lange Medical Books/McGraw-Hill, 2002:1203–1215.
   Google Scholar
• Rother KI. Diabetes treatment–bridging the divide. Engl J Med 2007;356:1499–1501.
   PubMed Web of Science ®Google Scholar
• Definition, Diagnosis and Classification of Diabetes Mellitus and its Complications. Geneva, World Health Organization Department of Noncommunicable Disease Surveillance 1999.
   Google Scholar
• Weiss J, Sumpio B. Review of prevalence and outcome of vascular disease in patients with diabetes mellitus. Eur J Vasc Endovasc Surg 2006;31:143–150.
   PubMed Web of Science ®Google Scholar
• Peek PM, Chrousos GP. Hypercortisolism and obesity. Ann NY Acad Sci 1995;771:665–676.
   PubMedGoogle Scholar
• Chapman KE, Coutinho A, Gray M, Gilmour JS, Savill JS, Secki JR. Local amplification of glucocorticoids by 11β-hydroxysteroid dehydrogenase type I and its role in inflammatory response. Ann NY Acad Sci 2006;1088:265–273.
   PubMed Web of Science ®Google Scholar
• Zhu Y, Olson SH, Graham D. Phenylcyclobutyl triazoles as selective inhibitors of 11β-hydroxysteroid dehydrogenase type. Bioorg Med Chem Lett 2008;18:3412–3416.
   PubMed Web of Science ®Google Scholar
• Ebdrup S, Sorensen LG, Olsen OH, Jacobsen P. Synthesis and structure–activity relationship for a novel class of potent and selective carbamoyl-triazole based inhibitors of hormone sensitive lipase. J Med Chem 2004;47:400–410.
   PubMedGoogle Scholar
• Strobl JS, Thomas MJ. Human growth hormone. Pharmacol Rev 1994;46:1–36.
   PubMed Web of Science ®Google Scholar
• Blenthen SL, Baptista J, Kuntze J, Foley T. Adult height in growth hormone (GH)-deficient children related with biosynthetic GH. J Clin Endocrinol Metab 1997;82:418–420.
   PubMedGoogle Scholar
• Bouillane O, Rainfray M, Tissandier O, Nasr A. Growth hormone therapy in elderly people: An age-delaying drug. Fundamen Clin Pharmacol 1996;10:416–430.
   PubMedGoogle Scholar
• Howard AD, Feighner SD, Cully DF, Arena JP. A receptor in pituitary and hypothalamus that functions in growth hormone release. Science 1996;273:974–977.
   PubMed Web of Science ®Google Scholar
• Stark D, Treiber HJ, Schobel D. Preparation of 3-[(aminoalkyl)thio]-1,2,4-triazoles on dopamine D3 receptors ligands. International patents WO 2000042038, 2000.
   Google Scholar
• Chan C, Dagnino R, Huang CQ, McCarthy JR. 1-Alkyl-3-amino-5-aryl-1H-[1,2,4-triazoles: novel synthesis via cyclization of N-acyl-S-methylisothoiureas with alkylhydrazines and their potent corticotrophin- releasing factor-1(CRF1) receptor antagonist activities. Bioorg Med Chem Lett 2001;11:3165–3168.
   PubMedGoogle Scholar
• Wandsworth HJ, Jenkins SM, Orlek BS, Casidy F, Brown F. Synthesis and muscarinic activities of quinuclidine-3-yl-triazole and tetrazole derivatives. J Med Chem 1992;35:1280–1290.
   PubMedGoogle Scholar
• Jenkins SM, Wandsworth HJ, Bromidge S, Orlek BS, Hawkins J. Substituent variation in azabicyclic triazole and tetrazole-based muscarinic receptor ligands. J Med Chem 1992;35:2392–2406.
   PubMed Web of Science ®Google Scholar
• Demange L, Boeglin D, Moulin A. Synthesis and pharmacological in vitro and in vivo evaluations of novel triazole derivatives as ligands of the ghrelin receptor-1. J Med Chem 2007;50:1939–1957.
   PubMed Web of Science ®Google Scholar
• Lang TJ. Estrogen as an immunomodulator. Clin Immunol 2004;113:224–230.
   PubMed Web of Science ®Google Scholar
• Gillett NA, Chan C. Applications of immunohistochemistry in the evaluation of immunosuppressive agents. Hum ExpToxicol 2000;19:251–254.
   PubMed Web of Science ®Google Scholar
• Lindstedt R, Ruggiero V, D′Alessio V, Manganello S, Petronzelli F, Stasi MA, Vendetti S, Assandri A, Carminati P, De Santis R. The immunosuppressor st1959, a 3,5-diaryl-s-triazole derivative, inhibits T cell activation by reducing NFAT nuclear residency. Int J Immunopathol Pharmacol 2009;22:29–42.
   PubMed Web of Science ®Google Scholar
• Sieh H. Oxidative stress: oxidants and antioxidants. Exp Physiol 1997;82;291–295.
   PubMedGoogle Scholar
• Aktay G, Tozkoparan B, Ertan M. Investigation of antioxidant properties of some 6-(alpha-aminobenzyl)thiazolo[3,2-b]-1,2,4-triazole-5-ol compounds. J Enzyme Inhib Med Chem 2008;27:1–5.
   Google Scholar
• Jankovic J. Parkinson′s disease: clinical features and diagnosis. J Neurol Neurosurg Psychiatr 2008;79:368–376.
   PubMed Web of Science ®Google Scholar
• Ongini E, Monopoli A, Cacciari B, Baraldi PG. Selective adenosine A2A receptor antagonist. Farmaco 2001;56:87–90.
   PubMedGoogle Scholar
• Gursoy A, Terzioglu N. Synthesis and isolation of new regioisomeric 4-thiazolidinones and their anticonvulsant activity. Turk J Chem 2005;29:247–254.
   Web of Science ®Google Scholar
• Pandeya SN, Sriram D, Yogeeswari P, Stables JP. Anticonvulsant and neurotoxicity evaluation of 5-(un)-substituted isatinimino derivatives. Pharmazie 2001;56:875–876.
   PubMedGoogle Scholar
• Karakurt A, Aytemir MD, Stables JP, Ozalp M, Betul Kaynak F, Ozbey S, Dalkara S. Synthesis of some oxime ether derivatives of 1-(2-naphthyl)-2-(1,2,4-triazol-1-yl)ethanone and their anticonvulsant and antimicrobial activities. Arch Pharm 2006;339:513–520.
   PubMed Web of Science ®Google Scholar
• Sun XY, Jin YZ, Li FN, Li G, Chai KY, Quan ZS. Synthesis of 8-alkoxy-4, 5-dihydro-[1,2,4]triazole[4,3-a]quinoline-1-ones and evaluation of their anticonvulsant properties. Arch Pharm Res 2006;29:1080–1085.
   PubMed Web of Science ®Google Scholar
• Husain A, Naseer MA, Sarafroz M. Synthesis and anticonvulsant activity of some novel fused heterocyclic 1,2,4-triazolo-[3,4-b]-1,3,4-thiadiazole derivatives. Acta Pol Pharm 2009;66:135–140.
   PubMed Web of Science ®Google Scholar
• Siddiqui N, Alam MS, Ahsan W. Synthesis, anticonvulsant and toxicity evaluation of 2-(1H-indol-3-yl)acetyl-N-(substituted phenyl)hydrazine carbothioamides and their related heterocyclic derivatives. Acta Pharm 2008;58:445–454.
   PubMed Web of Science ®Google Scholar
• Kucukguzel G, Kocatepe A, De Clercq E, Sahin F, Gulluce M. Synthesis and biological activity of 4-thiazolidinones, thiosemicarbazides derived from diflunisal hydrazide. Eur J Med Chem 2006;41:353–359.
   PubMed Web of Science ®Google Scholar
• Snider DE, Raviglione M Jr, Kochi A. Global burden of tuberculosis, chapter 1. In: Tuberculosis:Pathogenisis, Protection, and Control. American society for Microbiology, Washington, DC 20005.1994:3–11.
   Google Scholar
• Ballel L, Field RA, Duncan K, Young R. New small molecule synthetic antimycobacterials. Antimicrob Agents Chemotherapy 2005;49:2153–2163.
   PubMedGoogle Scholar
• Spigelman MK. New tuberculosis therapeutics: a growing pipeline. J Infect Dis 2007;196:528–536.
   PubMedGoogle Scholar
• Cottet F, Marull M, Lefebvre O. Recommendable routes to trifluoromethyl substituted pyridine and quinoline carboxylic acids. Eur J Org Chem 2003;8:1559–1568.
   Google Scholar
• Abdel-Rahman HM, El-Koussi NA, Hassan HY. Fluorinated 1,2,4-Triazolo[1,5-a]pyrimidine-6-carboxylic acid derivatives as antimycobacterial agents. Arch Pharm 2009;342:94–99.
   PubMed Web of Science ®Google Scholar
• Shiradkar M, Suresh Kumar GV, Dasari V, Tatikonda S, Akula KC, Shah R. Clubbed triazoles: a novel approach to antitubercular drugs Eur J Med Chem 2007;42:807–816.
   PubMed Web of Science ®Google Scholar
• Kaplancikli TA, Turan-Zitouni G, Chevallet P. Synthesis and antituberculosis activity of new 3-alkylsulfanyl-1,2,4-triazole derivatives. J Enzyme Inhib Med Chem 2005;20:179–182.
   PubMed Web of Science ®Google Scholar
• Upadhayaya RS, Kulkarni GM, Vasireddy NR, Vandavasi JK, Dixit SS, Sharma V, Chattopadhyaya J. Design, synthesis and biological evaluation of novel triazole, urea and thiourea derivatives of quinoline against Mycobacterium tuberculosis. Bioorg Med Chem 2009;17:4681–4692.
   PubMed Web of Science ®Google Scholar
• Jadhav GR, Shaikh MU, Kale RP, Shiradkar MR, Gill CH. SAR study of clubbed [1,2,4]-triazolyl with fluorobenzimidazoles as antimicrobial and antituberculosis agents. Eur J Med Chem 2009;44:2930–2935.
   PubMed Web of Science ®Google Scholar
• Barreca M L, Chimirri A, Luca LD, Monforte AM, Monforte P, Rao A, Zappala M, Balzarini J, Clercq ED, Pannecouque C, Witvrouw M. Discovery of 2,3-diaryl-1,3-thiazolidin-4-ones as potent anti-HIV-1 agents. Bioorg Med Chem Lett 2001;11:1793–1796.
   PubMedGoogle Scholar
• Rao A, Balzarini J, Carbone A, Chimirri A, Clercq ED, Monforte AM, Monforte P, Pannecouque C, Zappalà M. 2-(2,6-dihalophenyl)-3-(pyrimidin-2-yl)-1,3-thiazolidin-4-ones as non-nucleoside HIV-1 reverse transcriptase inhibitors. Antiviral Res 2004;63:79–84.
   PubMed Web of Science ®Google Scholar
• Rao A, Carbone A, Chimirri A, Clercq ED, Monforte AM, Monforte P, Pannecouque C, Zappala M. Synthesis and anti-HIV activity of 2,3-diaryl-1,3-thiazolidin-4-ones. Farmaco 2003;58:115–120.
   PubMedGoogle Scholar
• Wang Z, Wu B, Kuhen KL, Bursulaya B, Nguyen TN, Nguyen DG, He Y. Synthesis and biological evaluations of sulfanyltriazoles as novel HIV-1 non-nucleoside reverse transcriptase inhibitors. Bioorg Med Chem Lett 2006;16:4174–4177.
   PubMed Web of Science ®Google Scholar
• De La Rosa M, Kim HW, Gunic E, Jenket C, Boyle U, Koh YH., Korboukh I, Allan M, Zhang W, Chen H, Xu W, Nilar S, Yao N, Hamatake R, Lang SA, Hong Z, Zhang Z, Girardet JL. Tri-substituted triazoles as potent non-nucleoside inhibitors of HIV-1 reverse transcriptase. Bioorg Med Chem Lett 2006;16:4444–4449.
   PubMedGoogle Scholar
• Jordao AK, Afonso PP, Ferreira VF, De Souza MC, Almeida MC, Beltrame CO, Paiva DP, Wardell SM, Wardell JL, Tiekink ER, Damaso CR, Cunha AC. Antiviral evaluation of N-amino-1,2,3-triazoles against Cantagalo virus replication in cell culture. Eur J Med Chem 2009;44:3777–3783.
   PubMed Web of Science ®Google Scholar
• Carretero OA, Oparil S. Essential hypertension. Part I: Definition and etiology. Circulation 2000;101:329–335.
   PubMed Web of Science ®Google Scholar
• Guyton & Hall, and John E. Hall Textbook of Medical Physiology, 11th Edition, Elsevier 2005;7:220.
   Google Scholar
• Chobanian AV, Bakris GL, Black HR. Seventh report of the joint national committee on prevention, detection, evaluation, and treatment of high blood pressure. Hypertension 2003;42:1206–1252.
   PubMed Web of Science ®Google Scholar
• Kakefuda A, Suzuki T, Tobe T, Tsukada J, Tahara A, Sakamoto S, Tsukamoto S. Synthesis and pharmacological evaluation of 5-(4-biphenyl)-3-methyl-4-phenyl-1,2,4-triazole derivatives as a novel class of selective antagonists for the human vasopressin V(1A) receptor. J Med Chem 2002;45:2589–2598.
   PubMedGoogle Scholar
• Okazaki T, Suga A, Watanabe T, Kikuchi K, Kurihara H, Shibasaki M, Fujimori A, Inagaki O, Yanagisawa U. Studies on nonpeptide angiotensin II receptor antagonists I: Synthesis and biological evaluation of pyrazolo[1,5-b][1,2,4]triazole derivatives with alkyl substituents. Chem Pharm Bull 1998;46:69–78.
   PubMedGoogle Scholar
• Vega JA, Mortimer AM, Tyson PJ. Conventional antipsychotic prescription in unipolar depression, I: An audit and recommendations for practice. The Journal of clinical psychiatry 2003;64:568–574.
   PubMedGoogle Scholar
• Varvaresou A, Siatra-Papastaikoudi T, Dalla TA, Tsantili-Kakoulidou A, Vamvakides A. Synthesis, lipophilicity and biological evaluation of indole-containing derivatives of 1,3,4-thiadiazole and 1,2,4-triazole. Farmaco 1998;53:320–326.
   PubMedGoogle Scholar
• Roshan JB, Schulkin J. From fear to pathological anxiety. Psychol Rev 1998;105:325–350.
   PubMedGoogle Scholar
• Carling RW, Moore KW, Street LJ, Wild D, Isted C, Leeson PD, Thomas S, O′Connor D, McKernan RM, Quirk K, Cook SM, Atack JR, Wafford KA, Thompson SA, Dawson GR, Ferris P, Castro JL. 3-phenyl-6-(2-pyridyl)methyloxy-1,2,4-triazolo[3,4-a]phthalazines and analogues: high-affinity gamma-aminobutyric acid-A benzodiazepine receptor ligands with alpha 2, alpha 3, and alpha 5-subtype binding selectivity over alpha 1. J Med Chem 2004;47:1807–1822.
   PubMed Web of Science ®Google Scholar
• Akbarzadeh T, Tabatabai SA, Khoshnoud MJ, Shafaghi B, Shafiee A. Design and synthesis of 4H-3-(2-phenoxy)phenyl-1,2,4-triazole derivatives as benzodiazepine receptor agonists. Bioorg Med Chem 2003;11:769–773.
   PubMed Web of Science ®Google Scholar
• Carling RW, Madin A, Guiblin A, Russell MG, Moore KW, Mitchinson A, Sohal B, Pike A, Cook SM, Ragan IC, McKernan RM, Quirk K, Ferris P, Marshall G, Thompson SA, Wafford KA, Dawson GR, Atack JR, Harrison T, Castro JL, Street LJ. 7-(1,1-Dimethylethyl)-6-(2-ethyl-2H-1,2,4-triazol-3-ylmethoxy)-3-(2-fluorophenyl)-1,2,4-triazolo[4,3-b]pyridazine: a functionally selective gamma-aminobutyric acidA (GABAA) alpha2/alpha3-subtype selective agonist that exhibits potent anxiolytic activity but is not sedating in animal models. J Med Chem 2005;48:7089–7092.
   PubMed Web of Science ®Google Scholar
• Leurs R, Church MK, Taglialatela M. H1-antihistamines: inverse agonism, anti-inflammatory actions and cardiac effects. Clin Exp Allergy 2002;32:489–498.
   PubMed Web of Science ®Google Scholar
• Alagarsamy V, Sharma HK, Parthiban P, Singh JC, Murugan ST, Solomon VR. 4-(3-Methoxyphenyl)-1-substituted-4H-[1,2,4]triazolo[4,3-a]quinazolin-5-ones: new class of H1-antihistaminic agents. Pharmazie 2009;64:5–9.
   PubMedGoogle Scholar
• Alagarsamy V, Giridhar R, Yadav MR. Synthesis and pharmacological investigation of novel 1-substituted-4-phenyl-1,2,4-triazolo[4,3-a]quinazolin-5(4H)-ones as a new class of H1-antihistaminic agents. Bioorg Med Chem Lett 2005;15:1877–1880.
   PubMed Web of Science ®Google Scholar
• Fishbein M. Anesthesia. The New Illustrated Medical and Health Encyclopedia. amazon.co.uk 1976:87. 1976:87.
   Google Scholar
• Vazzana I, Boido A, Sparatore F, Di Carlo R, Raso GM, Pacilio M. Preparation and local anaesthetic activity of N-[2-(tert-amino)ethyl]- and N-(lupinyl)-benzotriazol-1/2-ylacetamides. Farmaco 1997;52:131–139.
   PubMedGoogle Scholar
• Snow RW, Guerra CA, Noor AM, Myint HY, Hay SI. The global distribution of clinical episodes of Plasmodium falciparum malaria. Nature 2005;434:214–217.
   PubMed Web of Science ®Google Scholar
• Mishra N, Arora P, Kumar B, Mishra LC, Bhattacharya A, Awasthi SK, Bhasin VK. Synthesis of novel substituted 1,3-diaryl propenone derivatives and their antimalarial activity in vitro. Eur J Med Chem 2008;43:1530–1535.
   PubMed Web of Science ®Google Scholar
• Tron GC, Pirali T, Billington RA, Canonico PL, Sorba G, Genazzani AA. Click chemistry reactions in medicinal chemistry: applications of the 1,3-dipolar cycloaddition between azides and alkynes. Med Res Rev 2008;28:278–308.
   PubMed Web of Science ®Google Scholar
• Wender PH, Handy ST, Wright DL. Towards the ideal synthesis. Chem Ind 1997;19:765–768.
   Google Scholar
• Kolb HC, Finn MG, Sharpless KB. Click chemistry: diverse chemical function from a few good reactions. Angew Chem Int Ed Engl 2001;40:2004–2021.
   PubMed Web of Science ®Google Scholar
• Kolb HC, Sharpless KB. The growing impact of click chemistry on drug discovery. Drug Discov Today 2003;8:1128–1137.
   PubMed Web of Science ®Google Scholar
• Appukkuttan P, Dehaen W, Fokin VV, Eycken D. A microwave-assisted click chemistry synthesis of 1,4-disubstituted 1,2,3-triazoles via a copper(I)-catalyzed three-component reaction. Org Lett 2004;6:4223–4225.
   PubMed Web of Science ®Google Scholar
• Feldman AK, Colasson B, Fokin VV. One-pot synthesis of 1,4-disubstituted 1,2,3-triazoles from in situ generated azides. Org Lett 2004;6:3897–3899.
   PubMed Web of Science ®Google Scholar
• Lee JW, Han SC, Kim JH, Ko YH, Kim K. Formation of rotaxane dendrimers by supramolecular click chemistry. Bull Kor Chem Soc 2007;28:1837–1840.
   Web of Science ®Google Scholar
• Cho M J, Cho MG, Huh SC, Kim SM, Lee K, Koh KO, Mang JY, Kim DY. Asymmetric Michael reaction of malonate derivatives with α,β-unsaturated ketones using chiral quaternary ammonium salts. Bull Kor Chem Soc 2006;27:857–862.
   Google Scholar
• Mammen M, Choi SK, George M. Polyvalent interactions in biological systems: implications for design and use of multivalent ligands and inhibitors. Angew Chem Int Ed Engl 1998;37:2754–2794.
   PubMed Web of Science ®Google Scholar
• Bennett I, Broom NJP, Bruton G, Calvert S, Clarke BP, Coleman K, Edmondson R, Edwards P, Jones D, Osborne NF, Walker G. 6-(substituted methylene)penenms, potent broad spectrum inhibitors of bacterial beta lactamase. J Antibiotics 1991;44:331–337.
   PubMed Web of Science ®Google Scholar
• Giffin MJ, Heaslet H, Brik A, Lin YC, Cauvi G. A copper (I)-catalyzed 1,2,3-triazole azide-alkyne click compound is a potent inhibitor of a multidrug-resistant HIV-1 protease variant. J Med Chem 2008;51:6263–6270.
   PubMed Web of Science ®Google Scholar
• Pagliai F, Pirali T, Grosso ED, Brisco RD, Tron GC, Sorba G, Genazzani AA. Rapid synthesis of triazole-modified resveratrol analogues via click chemistry. J Med Chem 2006;49:467–470.
   PubMed Web of Science ®Google Scholar
• Winum JV, Casini A, Mincione F, Starnotti M, Montero JL, Scozzafava A, Supuran C T. Carbonic anhydrase inhibitors: N-(p-sulfamoylphenyl)-α-D-glycopyranosylamines as topically acting antiglaucoma agents in hypertensive rabbits. Bioorg Med Chem Lett 2004;14:225–229.
   PubMed Web of Science ®Google Scholar
• Wilkinson BL, Bornaghi LF, Houston TA, Innocenti A, Supuran CT, Poulsen SA. A novel class of carbonic anhydrase inhibitors: glycoconjugate benzene sulfonamides prepared by “click-tailing”. J Med Chem 2006;49:6539–6548.
   PubMed Web of Science ®Google Scholar
• Chen Y, Lopez-Sanchez M, Savoy DN, Billadeau DD, Dow GS, Kozikowski AP. A series of potent and selective, triazolylphenyl-based histone deacetylases inhibitors with activity against pancreatic cancer cells and Plasmodium falciparum. J Med Chem 2008;51:3437–3448.
   PubMed Web of Science ®Google Scholar
• Kamal A, Shankaraiah N, Devaiah V, Reddy KL, Juvekar A, Sen S, Kurian N, Zingde S. Synthesis of 1,2,3-triazole-linked pyrrolobenzodiazepine (PBD) conjugates employing click chemistry: DNA-binding affinity and anticancer activity. Bioorg Med Chem Lett 2008;18:1468–1473.
   PubMed Web of Science ®Google Scholar
• Girmenia C. New generation azole antifungals in clinical investigation. Expert Opin Investig Drugs 2009;18:1279–1295.
   PubMed Web of Science ®Google Scholar
• Elia G, Belloli C, Cirone F. In vitro efficacy of ribavirin against canine distemper virus. Antiviral Res 2008;77:108–113.
   PubMed Web of Science ®Google Scholar
• Bani-Sadr F, Carrat F, Pol S. Risk factors for symptomatic mitochondrial toxicity in HIV/hepatitis C virus-coinfected patients during interferon plus ribavirin-based therapy. J Acquir Immune Defic Syndr 2005;40:47–52.
   PubMed Web of Science ®Google Scholar
• Alvarez D, Dieterich DT, Brau N, Moorehead L, Ball L, Sulkowski MS. Zidovudine use but not weight-based ribavirin dosing impacts anaemia during HCV treatment in HIV-infected persons. J Viral Hepat 2006;13:683–689.
   PubMed Web of Science ®Google Scholar
• Crotty S, Cameron C, Andino R. Ribavirin′s antiviral mechanism of action: lethal mutagenesis? J Mol Med 2002;80:86–95.
   PubMed Web of Science ®Google Scholar
• Bechir M, Schwegler K, Chenevard R. Anxiolytic therapy with alprazolam increases muscle sympathetic activity in patients with panic disorders. Auton Neurosci 2007;134:69–73.
   PubMedGoogle Scholar
• Skelton KH, Nemeroff CB, Owens MJ. Spontaneous withdrawal from the triazolobenzodiazepine alprazolam increases cortical corticotropin-releasing factor mRNA expression. J Neurosci 2004;24:9303–9312.
   PubMedGoogle Scholar
• Wolf BC, Lavezzi WA, Sullivan LM, Middleberg RA, Flannagan LM. Alprazolam-related deaths in Palm Beach County. Am J Forensic Med Pathol 2005;26:24–27.
   PubMed Web of Science ®Google Scholar
• Miura M, Otani K, Ohkubo T. Identification of human cytochrome P450 enzymes involved in the formation of 4-hydroxyestazolam from estazolam. Xenobiotica 2005;35:455–465.
   PubMed Web of Science ®Google Scholar
• Hakimian S, Cheng-Hakimian A, Anderson GD, Miller JW. Rufinamide: a new anti-epileptic medication. Expert Opin Pharmacother 2007;8:1931–1940.
   PubMed Web of Science ®Google Scholar
• Borras L, De Timary P, Constant EL, Huguelet P, Eytan A. Successful treatment of alcohol withdrawal with trazodone. Pharmacopsychiatry 2006;39:232.
   PubMedGoogle Scholar
• Saper JR, Lake AE, Tepper SJ. Nefazodone for chronic daily headache prophylaxis: an open-label study. Headache 2001;41:465–474.
   PubMed Web of Science ®Google Scholar
• Rachwalski EJ, Wieczorkiewicz JT, Scheetz MH. Posaconazole: an oral triazole with an extended spectrum of activity. Ann Pharmacother 2008;42:1429–1438.
   PubMed Web of Science ®Google Scholar
• Cornely O, Maertens J, Winston D, Perfect J, Ullmann A, Walsh T, Helfgott D, Holowiecki J, Stockelberg D, Goh Y, Petrini M, Hardalo C, Suresh R, Angulo-Gonzalez D. Posaconazole versus fluconazole or itraconazole prophylaxis in patients with neutropenia. N Engl J Med 2007;356:348–359.
   PubMed Web of Science ®Google Scholar
• Ullmann A, Lipton J, Vesole D, Chandrasekar P, Langston A, Tarantolo S, Greinix H, Morais de Azevedo W, Reddy V, Boparai N, Pedicone L, Patino H, Durrant S. Posaconazole or fluconazole for prophylaxis in severe graft-versus-host disease. N Engl J Med 2007;356:335–347.
   PubMed Web of Science ®Google Scholar
• Smith J, Safdar N, Knasinski V, Simmons W, Bhavnani S, Ambrose P, Andes D. Voriconazole therapeutic drug monitoring. Antimicrob Agents Chemother 2006;50:1570–1572.
   PubMed Web of Science ®Google Scholar