Optimization of the beta-aminoester class of factor Xa inhibitors. Part 1: P(4) and side-chain modifications for improved in vitro potency.
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Czekaj M, Klein SI, Guertin KR, Gardner CJ, Zulli AL, Pauls HW, Spada AP, Cheney DL, Brown KD, Colussi DJ, Chu V, Leadley RJ, Dunwiddie CT
Optimization of the beta-aminoester class of factor Xa inhibitors. Part 1: P(4) and side-chain modifications for improved in vitro potency.
Bioorg Med Chem Lett. 2002 Jun 17;12(12):1667-70.
- PubMed ID
- 12039586 [ View in PubMed]
- Abstract
A systematic modification of the C(3) side-chain of the beta-aminoester class of factor Xa inhibitors and a survey of P(4) variations is described. These changes have resulted in the identification of sub-nanomolar inhibitors with improved selectivity versus related proteases. Coagulation parameters (i.e., APTT doubling concentrations) are also improved.