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Optimization of the beta-aminoester class of factor Xa inhibitors. Part 1: P(4) and side-chain modifications for improved in vitro potency.
Czekaj, Mark; Klein, Scott I; Guertin, Kevin R; Gardner, Charles J; Zulli, Allison L; Pauls, Henry W; Spada, Alfred P; Cheney, Daniel L; Brown, Karen D; Colussi, Dennis J; Chu, Valeria; Leadley, Robert J; Dunwiddie, Christopher T.
Afiliação
  • Czekaj M; Drug Innovation and Approval, Aventis Pharmaceuticals, Route 202-206, Bridgewater, NJ 08807, USA. mark.czekaj@aventis.com
Bioorg Med Chem Lett ; 12(12): 1667-70, 2002 Jun 17.
Article em En | MEDLINE | ID: mdl-12039586
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.
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Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Inibidores de Serina Proteinase / Inibidores do Fator Xa Tipo de estudo: Prognostic_studies Idioma: En Ano de publicação: 2002 Tipo de documento: Article
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Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Inibidores de Serina Proteinase / Inibidores do Fator Xa Tipo de estudo: Prognostic_studies Idioma: En Ano de publicação: 2002 Tipo de documento: Article