Ketene aminal-based lactam derivatives as a novel class of orally active FXa inhibitors.

Shi, Yan; Zhang, Jing; Stein, Philip D; Shi, Mengxiao; O'Connor, Stephen P; Bisaha, Sharon N; Li, Chi; Atwal, Karnail S; Bisacchi, Gregory S; Sitkoff, Doree; Pudzianowski, Andrew T; Liu, Eddie C; Hartl, Karen S; Seiler, Steven M; Youssef, Sonia; Steinbacher, Thomas E; Schumacher, William A; Rendina, Alan R; Bozarth, Jeffrey M; Peterson, Tara L; Zhang, Ge; Zahler, Robert

Shi, Yan; Zhang, Jing; Stein, Philip D; Shi, Mengxiao; O'Connor, Stephen P; Bisaha, Sharon N; Li, Chi; Atwal, Karnail S; Bisacchi, Gregory S; Sitkoff, Doree; Pudzianowski, Andrew T; Liu, Eddie C; Hartl, Karen S; Seiler, Steven M; Youssef, Sonia; Steinbacher, Thomas E; Schumacher, William A; Rendina, Alan R; Bozarth, Jeffrey M; Peterson, Tara L; Zhang, Ge; Zahler, Robert.

Afiliação

Shi Y; Bristol-Myers Squibb Pharmaceutical Research Institute, PO Box 5400, Princeton, NJ 08543-5400, USA. yan.shi@bms.com

Bioorg Med Chem Lett ; 15(24): 5453-8, 2005 Dec 15.

Article em En | MEDLINE | ID: mdl-16213711

ABSTRACT

ABSTRACT

N,N'-Disubstituted ketene aminals are good bioisosteres of thiourea functional groups. We report the design and synthesis of a novel class of ketene aminal-based lactam derivatives as potent and orally active FXa inhibitors.

Assuntos

Etilenos/farmacologia; Inibidores do Fator Xa; Cetonas/farmacologia; Lactamas/farmacologia; Administração Oral; Etilenos/administração & dosagem; Etilenos/química; Humanos; Cetonas/administração & dosagem; Cetonas/química; Lactamas/administração & dosagem; Modelos Moleculares; Conformação Molecular; Relação Estrutura-Atividade

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Base de dados: MEDLINE Assunto principal: Etilenos / Inibidores do Fator Xa / Cetonas / Lactamas Tipo de estudo: Prognostic_studies Limite: Humans Idioma: En Ano de publicação: 2005 Tipo de documento: Article

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