ChemInform Abstract: Diamino Benzo[b]thiophene Derivatives as a Novel Class of Active Site Directed Thrombin Inhibitors. Part 5. Potency, Efficacy, and Pharmacokinetic Properties of Modified C-3 Side Chain Derivatives.
Abstract
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ChemInform Abstract
A systematic structure—activity relationship study surrounding the C-3 side chain of a structurally novel class of benzothiophene thrombin inhibitors is reported. These investigations lead to the potent thrombin inhibitors (VI), (X) and (XIII) with levels of thrombin selectivity which are among the highest yet reported. However, the efficacy of these compounds is currently limited by their rapid and extensive distribution following administration.