PNEUMOCANDIN ANTIFUNGAL LIPOPEPTIDES - THE PHENOLIC HYDROXYL IS REQUIRED FOR 1,3-BETA-GLUCAN SYNTHESIS INHIBITION

被引：18

作者：

BALKOVEC, JM

BLACK, RM

ABRUZZO, GK

BARTIZAL, K

DREIKORN, S

NOLLSTADT, K

机构：

[1] MERCK RES LABS, DEPT BIOCHEM PARASITOL, RAHWAY, NJ 07065 USA

[2] MERCK RES LABS, DEPT MICROBIOL, RAHWAY, NJ 07065 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1993年 / 3卷 / 10期

关键词：

D O I：

10.1016/S0960-894X(01)81010-6

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Pneumocandin B-0 1 undergoes selective oxidation/reduction chemistry at the homotyrosine (hty) residue. Removal of the phenolic hydroxyl gives >140-fold loss in activity against a Candida albicans 1,3-beta-glucan synthetase enzyme preparation and a significant loss of antifungal activity. Inversion of the C4-hty hydroxyl causes about a 70-fold decrease in potency, while removal of this hydroxyl yields a more potent inhibitor.

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页码：2039 / 2042

页数：4

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