1. Anthranilamide inhibitors of factor Xa.
- Author
-
Mendel D, Marquart AL, Joseph S, Waid P, Yee YK, Tebbe AL, Ratz AM, Herron DK, Goodson T, Masters JJ, Franciskovich JB, Tinsley JM, Wiley MR, Weir LC, Kyle JA, Klimkowski VJ, Smith GF, Towner RD, Froelich LL, Buben J, and Craft TJ
- Subjects
- Anticoagulants chemistry, Antithrombin III chemistry, Binding Sites, Chemistry, Pharmaceutical methods, Dose-Response Relationship, Drug, Drug Design, Drug Evaluation, Preclinical, Fluorescent Dyes chemical synthesis, Humans, Kinetics, Models, Chemical, Molecular Conformation, Structure-Activity Relationship, ortho-Aminobenzoates chemical synthesis, Antithrombin III chemical synthesis, Factor Xa Inhibitors, Fluorescent Dyes pharmacology, ortho-Aminobenzoates pharmacology
- Abstract
SAR about the B-ring of a series of N(2)-aroyl anthranilamide factor Xa (fXa) inhibitors is described. B-ring o-aminoalkylether and B-ring p-amine probes of the S1' and S4 sites, respectively, afforded picomolar fXa inhibitors that performed well in in vitro anticoagulation assays.
- Published
- 2007
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