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L-373,890, An achiral, noncovalent, subnanomolar thrombin inhibitor

Authors
Journal
Bioorganic & Medicinal Chemistry Letters
0960-894X
Publisher
Elsevier
Publication Date
Volume
7
Issue
12
Identifiers
DOI: 10.1016/s0960-894x(97)00257-6
Disciplines
  • Design

Abstract

In the first successful application of the 3-aminopyridinone acetamide template for the synthesis of a potent, noncovalent inhibitor of either a cysteine or a serine protease, L-373,890, a highly selective and efficacious thrombin inhibitor was designed using a combination of X-ray crystallography, molecular modeling, and empirical structure optimization.

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