Synthesis and structure-activity relationships of novel 3'-HTY-substituted pneumocandins

被引：10
|
作者：
Black, RM
Balkovec, JM
Nollstadt, KM
Dreikorn, S
Bartizal, KF
Abruzzo, GK
机构：
[1] MERCK RES LABS,DEPT PARASITE BIOCHEM & CELL BIOL,RAHWAY,NJ 07065
[2] MERCK RES LABS,DEPT ANTIBIOT DISCOVERY & DEV,RAHWAY,NJ 07065
[3] MERCK RES LABS,DEPT INFECT DIS RES,RAHWAY,NJ 07065
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1997年 / 7卷 / 22期
关键词：
D O I：
10.1016/S0960-894X(97)10107-X
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A series of pneumocandin B-0 analogs substituted at the 3'-position of the homotyrosine (Hty) residue have been prepared and evaluated for their inhibition of 1,3-beta-(D)-glucan synthesis and for their antifungal activity against C. albicans. Cationic analogs displayed enhanced antifungal properties. The phenolic hydroxyl is involved in a critical hydrogen-bond at the binding site of the enzyme. (C) 1997 Elsevier Science Ltd.
引用
收藏
页码：2879 / 2884
页数：6
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