Structure-activity relationship of a series of phenylureas linked to 4-phenylimidazole. Novel potent inhibitors of acyl-CoA: cholesterol O-acyltransferase with …

…, K Hayashi, H Tanaka, I Ohtsuka, T Saeki…

Index: Kimura; Watanabe; Matsui; Hayashi; Tanaka; Ohtsuka; Saeki; Kogushi; Kabayashi; Akasaka; Yamagishi; Saitou; Yamatsu Journal of Medicinal Chemistry, 1993 , vol. 36, # 11 p. 1641 - 1653

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Citation Number: 19

Abstract

In our continuing search to find systemically bioavailable ACAT (acyl-CoAcholesterol 0- acyltransferase) inhibitors with more potent antiatherosclerotic effect than N-[2- (dimethylamino)-6-[3-(5-methyl-4-phenyl-l~-imidazol-l-yl) propoxylphenyll-N'-pentylurea (3), a series of phenyl-ureas linked to 4-phenylimidazole were synthesized and evaluated for in vitro inhibitory activity toward both aortic and intestinal ACATs, and for in vivo ...