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Tetrazole-substituted ureas as inhibitors of acyl-CoA:cholesterol O-acyltransferase (ACAT). A novel preparation of ureas from weakly nucleophilic amines

✍ Scribed by Claude F Purchase II; Andrew D White; Maureen K Anderson; Thomas M.A Bocan; Richard F Bousley; Katherine L Hamelehle; Reynold Homan; Brian R Krause; Peter Lee; Sandra Bak Mueller; Cecilia Speyer; Richard L Stanfield; James F Reindel

Book ID: 103983479
Publisher: Elsevier Science
Year: 1996
Tongue: English
Weight: 327 KB
Volume: 6
Category: Article
ISSN: 0960-894X
DOI: 10.1016/0960-894x(96)00310-1

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✦ Synopsis

A novel series of tetrazole-substituted ureas 2 were prepared from weakly nucleophilic amines using a new coupling method. The ureas were found to potently inhibit liver ACAT in vitro and lower total serum cholesterol in vivo. A comparison of urea 2b and the anti-atherosclerotic CI-976 in a long-term model of atherosclerosis indicates the importance of inhibiting arterial ACAT for reducing lesion size.

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