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.

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页码：2879 / 2884

页数：6

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