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Structure-activity relationship of N-[2-(dimethylamino)-6-[3-(5-methyl-4-phenyl-1H-imidazol-1-yl) propoxy] phenyl]-N'-pentylurea and analogs. Novel potent inhibitors of …

…, I Ohtsuka, T Saeki, M Kogushi, T Yamada…

文献索引:Kimura; Takase; Hayashi; Tanaka; Ohtsuka; Saeki; Kogushi; Yamada; Fujimori; Saitou; Akasaka Journal of Medicinal Chemistry, 1993 , vol. 36, # 11 p. 1630 - 1640

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被引用次数: 26

摘要

We have discovered N-butyl-N'-[2-(dimethylamino)-6-[3-(4-phenyl-1H-imidazol-l-yl) propoxy]- phenyl] urea (4), a novel, potent, and systemically bioavailable inhibitor of ACAT (acylCoA: cholesterol 0-acyltransferase). The structure-activity relationships (SARs) of this lead compound 4 were investigated by systematic modification of four regions in the molecule. The compounds prepared in this study were tested for in vitro inhibitory activity toward ...