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Abstract
Novelty: An antibiotic compound, 1 -[4-hydroxy-5-aminoethyloxy-N2-(10.12-dimethyl-1-oxotetradecyl)omithine]-5-(3-hydroxyglu~mine)-6-(3-hydroxyproline)echinocandin B, is disclosed. The compound has potential in the therapy of human mycotic infections and may be used for inhibiting or alleviating Pneurnacysris carinii infections, prevalent in immuno compromised patients.
Biology: The antifungal ability of the compound was determined against many strains using microbroth dilution assay. Results showed the minimal fungicidal concentration against Candida albicans MY 1055 was 0.125 μg/ml. The lytic activity of the compound was also assayed. The minimum lytic concentration to produce complete or partial lysis of red blood cells was 400 mg/ml.
Chemistry: The process for the preparation of the compound comprises reacting 1 -[4,5-dihydroxy-N2-(10,12-dimethyl-1-oxotetradecyl)ornithineJ-5-(3-hydroxy-glutamine)-6-(3-hydr-oxypro1ine)echinocandin B with ethanolamine hydrochloride, in the presence of strong acid in an aprotic polar solvent.