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

Article abstract of DOI:10.1016/S0960-894X(98)00143-7

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.