Volume 31, Issue 23
Heterocyclic Compounds
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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.

Daniel J. Sall

Daniel J. Sall

Lilly Res. Lab., Lilly Corp. Cent., Eli Lilly Co., Indianapolis, IN 46285, USA

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et al. et al.

et al. et al.

Lilly Res. Lab., Lilly Corp. Cent., Eli Lilly Co., Indianapolis, IN 46285, USA

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First published: 08 June 2010

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.

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