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ANTI-CRYPTOCOCCAL PEPTIDES

机译:抗隐球菌肽

摘要

Antifungals based on dolasatin 10 and four structural modifications thereof (herein "peptides") and methods of treating a host afflicted with a fungi-induced infection are herein described. In broth macrodilution assays, these peptides were fungicidal for ATCC stains and clinical isolates of Cryptococcus neoformans. Specificity for C. neoformans was also demonstrated in the solid-phase disk diffusion assay, and fungicidal activity confirmed in killing kinetics experiments. Broth macrodilution minimum inhibitory and minimum fungicidal concentrations for the most potent modification ranged from 0.0975-1.56 mug/ml and 0.0975-6.24 mug/ml respectively. The minimum inhibitory concentrations were nearly identical in the presence of human serum, but increased with lowered pH. Suitable dosage forms for use of the novel antifungals are also described.
机译:本文描述了基于d​​olasatin 10及其四个结构修饰的抗真菌剂(以下简称“肽”)以及治疗受真菌诱导感染的宿主的方法。在肉汤大量稀释测定中,这些肽对ATCC染色剂和新隐球菌的临床分离株具有杀真菌作用。在固相圆盘扩散试验中还证明了对新孢梭菌的特异性,并且在杀灭动力学实验中证实了杀真菌活性。最有效的修饰液的肉汤大量稀释的最小抑菌和最小杀真菌浓度分别为0.0975-1.56个/ ml和0.0975-6.24个/ ml。在人血清中,最低抑菌浓度几乎相同,但随着pH降低而增加。还描述了使用新型抗真菌剂的合适剂型。

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