Replacements for lysine in L-seryl-L-lysyl dipeptide amide inhibitors of Candida albicans myristoyl-CoA: Protein N-myristoyltransferase

被引：11

作者：

Brown, DL ^{[1
]}

Devadas, B ^{[1
]}

Lu, HF ^{[1
]}

Nagarajan, S ^{[1
]}

Zupec, ME ^{[1
]}

Freeman, SK ^{[1
]}

McWherter, CA ^{[1
]}

Getman, DP ^{[1
]}

Sikorski, JA ^{[1
]}

机构：

[1] GD SEARLE & CO,DEPT MED & STRUCT CHEM,ST LOUIS,MO 63198

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1997年 / 7卷 / 03期

关键词：

D O I：

10.1016/S0960-894X(97)00030-9

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A survey of potential cyclic and acyclic lysine replacements in known L-seryl-L-lysyl dipeptide inhibitors of C. albicans NMT identified the thioether 16 and glycinamide 18 as submicromolar inhibitors of C. albicans NMT, which retained goad selectivity over the human enzyme. Al of the heterocyclic lysine mimetics that were examined exhibited dramatically weaker affinity with the fungal enzyme. (C) 1997, Elsevier Science Ltd.

引用

页码：379 / 382

页数：4

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