含3-酰胺基的假霉素类似物的前药：新型抗真菌剂。
Prodrugs of 3-amido bearing pseudomycin analogues: novel antifungal agents.
作者信息
Sun X, Zeckner D, Zhang Y, Sachs R K, Current W L, Rodriguez M, Chen S H
机构信息
Lilly Research Laboratory, A Division of Eli Lilly and Company, Lilly Corporate Center, IN 46285, Indianapolis, USA.
出版信息
Bioorg Med Chem Lett. 2001 Jul 23;11(14):1881-4. doi: 10.1016/s0960-894x(01)00335-3.
With the aim of identifying safer pseudomycin derivatives, we synthesized and evaluated a number of N-acyloxymethyl carbamate linked prodrugs of 3-amido pseudomycin analogues. To our satisfaction, all of the prodrug-amide combinations prepared exhibited good in vivo efficacy against murine Candidiasis. When evaluated in a dose elevation study, all of the newly synthesized combinations (e.g., 4A, 6A, 8A, and 8B) demonstrated improved toxicity profiles in comparison to their corresponding 3-amides as well as the parent pseudomycin B.
为了鉴定更安全的假霉素衍生物，我们合成并评估了多种与3-氨基假霉素类似物相连的N-酰氧基甲基氨基甲酸酯前药。令我们满意的是，所制备的所有前药-酰胺组合对小鼠念珠菌病均表现出良好的体内疗效。在剂量递增研究中进行评估时，所有新合成的组合（例如4A、6A、8A和8B）与其相应的3-酰胺以及母体假霉素B相比，均表现出改善的毒性特征。
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