A series of conformationally and sterically constrained analogs of N-phenyl-N′-aralkylurea ACAT inhibitors

doi:10.1016/0960-894X(95)00387-9

Bioorganic & Medicinal Chemistry Letters

Volume 5, Issue 19, 5 October 1995, Pages 2229-2234

https://doi.org/10.1016/0960-894X(95)00387-9 Get rights and content

Abstract

A series of conformationally and sterically constrained analogs of N-phenyl-N′-aralkylureas has been synthesized and evaluated as potential ACAT inhibitors. Most of these analogs are potent inhibitors of ACAT in vitro and lower plasma cholesterol in an acute in vivo model of hypercholesterolemia.

A series of conformationally and sterically constrained analogs of N-phenyl-N'-aralkylureas has been synthesized which potently inhibit ACAT in vitro, and are efficacious cholesterol lowering agents in vivo.

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^☆: Inhibitors of Acyl-CoA:Cholesterol Acyl Transferase. Part 16. Presented in part at the 201st National ACS Meeting, Atlanta, Georgia,1991, MEDI 112. Stoeber, T. L.; Holmes A.; Essenburg, A. D.; Hamelehle, K. L.; Shaw, M. K.; Stanfield, R. L.; Krause, B. R.; Trivedi, B. K. A Series of Novel Disubstituted Ureas as ACAT Inhibitors: Chemistry and SAR Studies.

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A series of conformationally and sterically constrained analogs of N-phenyl-N′-aralkylurea ACAT inhibitors☆

Abstract

J. Biol. Chem.

Atherosclerosis

Current Op. Ther. Patents

Current Op. Ther. Patents

Current Med. Chem.