Synthetic [5,5] Trans-Fused Indane Lactones As Inhibitors Of Thrombin

M Pass,R E Bolton,S J Coote,H Finch,S Hindley,A Lowdon,E McDonald,J McLaren,M Owen,N A Pegg,C J Mooney,C M Tang,S Parry,C Patel

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS（1999）

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摘要

Synthesis of trans-fused lactones containing; the indane nucleus has resulted in a series of potent acylating inhibitors of thrombin. As an er;ample compound Ile has an apparent second order rate constant of 11x10(6) M(-1)sec(-1) for the inhibition of thrombin. The anticoagulant activity of these compounds is discussed. (C) 1999 Elsevier Science Ltd. All rights reserved.

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rate constant,second order

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