SCH 53823 and SCH 53825, novel fungal metabolites with phospholipase D inhibitory activity

被引：27

作者：

Chu, M

Patel, MG

Pai, JK

Das, PR

Puar, MS

机构：

[1] Schering-Plough Research Institute, Kenilworth, NJ 07033

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1996年 / 6卷 / 05期

关键词：

D O I：

10.1016/0960-894X(96)00074-1

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Two novel phospholipase D (PLD) inhibitors, Sch 53823 (1) and Sch 53825 (2), were isolated from a fungal culture. The acetylated derivatives, Sch 53827 (3) and Sch 53829 (4), were prepared for the purpose of structure determination. The extensive NMR studies of 3 and 4 including DEFT, COSY, NOESY, HETCOR, and selective INEPT experiments permitted the establishment of their structures, as well as relative stereochemistries. Among these compounds, 3 exhibited the most potent inhibitory activity in the phospholipase D assay with the IC50 = 17 mu M.

引用

页码：579 / 584

页数：6

共 11 条

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