Synthetic [5,5] trans-fused indane lactones as inhibitors of thrombin

Article abstract of DOI:10.1016/S0960-894X(99)00002-5

Synthesis of trans-fused lactones containing the indane nucleus has resulted in a series of potent acylating inhibitors of thrombin. As an example compound 11e has an apparent second order rate constant of 11 x 10⁶ M^-1 sec^-1 for the inhibition of thrombin. The anticoagulant activity of these compounds is discussed.