Inhibitors of acyl-CoA: cholesterol acyltransferase. 1. Synthesis and hypocholesterolemic activity of dibenz [b, e] oxepin-11-carboxanilides

T Kumazawa, M Yanase, H Harakawa…

Index: Kumazawa, Toshiaki; Yanase, Masashi; Harakawa, Hiroyuki; Obase, Hiroyuki; Shirakura, Shiro; et al. Journal of Medicinal Chemistry, 1994 , vol. 37, # 6 p. 804 - 810

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Citation Number: 26

Abstract

A series of N-phenyl-6, 11-dihydrodibenz [b, eloxepin-ll-carboxamides and related derivatives were prepared on the basis of structures of the reported inhibitors of acyl- CoAcholesterol acyltransferase (ACAT). These compounds were tested for their ability to inhibit ACAT (liver microsomes from cholesterol-fed rabbits) in vitro and to decrease serum total cholesterol in cholesterol-fed golden hamsters in vivo. The structure-activity ...