Cyclopentanedi-and tricarboxylic acids as squalene synthase inhibitors: syntheses and evaluation

…, DS Garvey, J Cohen, H Stein, SH Rosenberg

Index: Shen, Wang; Garvey, David S.; Cohen, Jerry; Stein, Herman; Rosenberg, Saul H. Bioorganic and Medicinal Chemistry Letters, 1998 , vol. 8, # 8 p. 891 - 896

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Citation Number: 6

Abstract

Based on earlier lead squalene synthase inhibitor A-87049 (3) and zaragozic acids, a series of cyclopentanedi-and tricarboxylic acids were synthesized and evaluated against the enzyme. Some exhibited good potency and SAR revealed the importance of conformation and substitution pattern of these synthetic inhibitors.