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Neutral inhibitors of the serine protease factor Xa
W D Shrader1, W B Young, P A Sprengeler
1Departments of Medicinal Chemistry, Structural Chemistry and Enzymology, Axys Pharmaceuticals, Inc., 180 Kimball Way, 94080, South San Francisco, CA, USA.
Bioorganic & Medicinal Chemistry Letters
|July 19, 2001
Abstract:
A neutral inhibitor of the serine protease factor Xa was identified via a high-throughput screen of a commercial library. The initial lead 1 demonstrated reversible and competitive inhibition kinetics for factor Xa and possessed a high degree of selectivity versus other related serine proteases. Initial modeling efforts and the generation of a series of analogues of 1 are described.