THE ISOLATION AND STRUCTURE ELUCIDATION OF ZARAGOZIC ACID-C, A NOVEL POTENT SQUALENE SYNTHASE INHIBITOR

被引:58
|
作者
DUFRESNE, C
WILSON, KE
ZINK, D
SMITH, J
BERGSTROM, JD
KURTZ, M
REW, D
NALLIN, M
JENKINS, R
BARTIZAL, K
TRAINOR, C
BILLS, G
MEINZ, M
HUANG, LY
ONISHI, J
MILLIGAN, J
MOJENA, M
PELAEZ, F
机构
[1] Merck Research Laboratories, Rahway, NJ 07065
关键词
D O I
10.1016/S0040-4020(01)88327-7
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
The novel zaragozic acid C (1) has been isolated as a potent inhibitor of squalene synthase. It was found to be a competitive inhibitor of rat lover squalene synthase with an apparent K(i) of 45 +/- 15 pM, and a broad spectrum antifungal agent against both yeast and filamentous fungi.
引用
收藏
页码:10221 / 10226
页数:6
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