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The de novo design and synthesis of cyclic urea inhibitors of factor Xa: optimization of the S4 ligand

✍ Scribed by Robert A. Galemmo Jr.; Brian L. Wells; Karen A. Rossi; Richard S. Alexander; Celia Dominguez; Thomas P. Maduskuie; Pieter F.W. Stouten; Matthew R. Wright; Bruce J. Aungst; Pancras C. Wong; Robert M. Knabb; Ruth R. Wexler

Book ID: 104364970
Publisher: Elsevier Science
Year: 2000
Tongue: English
Weight: 222 KB
Volume: 10
Category: Article
ISSN: 0960-894X
DOI: 10.1016/s0960-894x(99)00688-5

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✦ Synopsis

In this report refinements to the S4 ligand group leads to compound 19, an inhibitor of fXa with good potency in vitro and an improved pharmacokinetic profile in rabbit. The X-ray crystallographic study of a representative analogue confirms our binding model for this series.

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