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