2-CHLORO-1-(2,4-DICHLOROPHENYL)-3-(1H-IMIDAZOL-1-YL)-2-PHENYLPROPAN-1-ONE HYDROCHLORIDE, A NOVEL, NONMUTAGENIC ANTIBACTERIAL WITH SPECIFIC ACTIVITY AGAINST ANAEROBIC-BACTERIA

被引：11
|
作者：
DICKENS, JP
ELLAMES, GJ
HARE, NJ
LAWSON, KR
MCKAY, WR
METTERS, AP
MYERS, PL
POPE, AMS
UPTON, RM
机构：
[1] SEARLE RES & DEV,DEPT MED CHEM,HIGH WYCOMBE,BUCKS,ENGLAND
[2] SEARLE RES & DEV,DEPT BIOL,HIGH WYCOMBE,BUCKS,ENGLAND
来源：
JOURNAL OF MEDICINAL CHEMISTRY | 1991年 / 34卷 / 08期
关键词：
D O I：
10.1021/jm00112a006
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
1-(2,4-Dichlorophenyl)-2-phenylpropen-1-one (2) is identified as a potent antibacterial agent. A compound, 2-chloro-1-(2,4-dichlorophenyl)-3-(1H-imidazol-1-yl)-2-phenylpropan-1-one (5) has been designed with the intention of its acting as a pro-drug, liberating the lethal species 2 specifically within the target anaerobic bacterial cell following bioreduction by bacterial ferredoxin or related electron transfer proteins. The synthesis and biological activity of 5 is described and compared with the activities of the analogous alpha-bromo ketone 6 and alpha-fluoro ketone 7. Synthesis of 6, 7, and the corresponding alpha-hydroxy ketone 11 is also described.
引用
收藏
页码：2356 / 2360
页数：5
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