SYNTHESIS OF 1233A ANALOGS AND THEIR INHIBITORY ACTIVITY AGAINST HYDROXYMETHYLGLUTARYL COENZYME A SYNTHASE

被引:21
作者
SUNAZUKA, T
TSUZUKI, K
KUMAGAI, H
TOMODA, H
TANAKA, H
NAGASHIMA, H
HASHIZUME, H
OMURA, S
机构
[1] KITASATO INST,BIOL FUNCT RES CTR,MINATO KU,TOKYO 108,JAPAN
[2] DAHCHI PHARMACEUT CO LTD,EDOGAWA KU,TOKYO 134,JAPAN
[3] FUJI CHEM IND CO LTD,TAKAOKA,TOYAMA 933,JAPAN
[4] KITASATO UNIV,SCH PHARMACEUT SCI,MINATO KU,TOKYO 108,JAPAN
关键词
D O I
10.7164/antibiotics.45.1139
中图分类号
Q81 [生物工程学(生物技术)]; Q93 [微生物学];
学科分类号
071005 ; 0836 ; 090102 ; 100705 ;
摘要
Simple and efficient syntheses of 1233A analogs were developed and the inhibitory activity of the analogs against hydroxymethylglutaryl coenzyme A (HMG-CoA) synthase was determined. Study of the structure-activity relationships revealed that not only the geometry in beta-lactone moiety but also the length of the carbon side chain is important for inhibitory activity against HMG-CoA synthase.
引用
收藏
页码:1139 / 1147
页数:9
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