Substituted (1, 2-diarylethyl) amide acyl-CoA: cholesterol acyltransferase inhibitors: effect of polar groups on in vitro and in vivo activity

…, RE Burrier, HR Davis, M Domalski…

Index: Clader, John W.; Berger, Joel G.; Burrier, Robert E.; Davis, Harry R.; Domalski, Martin; et al. Journal of Medicinal Chemistry, 1995 , vol. 38, # 10 p. 1600 - 1607

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Citation Number: 41

Abstract

Substituted (1, 2-diarylethyl) amides have been prepared and evaluated for their ability to inhibit microsomal acyl-CoAcholesterol acyltransferase activity in vitro and to lower hepatic cholesteryl ester content in vivo in a cholesterol-fed hamster. Simple unsubstituted (diarylethy1) amides were potent inhibitors in vitro but showed poor activity in vivo. Introduction of polar groups at specific locations on the diarylethylamine moiety decreased ...