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Macrocyclic factor XIa inhibitors.
Wang, Cailan; Corte, James R; Rossi, Karen A; Bozarth, Jeffrey M; Wu, Yiming; Sheriff, Steven; Myers, Joseph E; Luettgen, Joseph M; Seiffert, Dietmar A; Wexler, Ruth R; Quan, Mimi L.
Afiliação
  • Wang C; Bristol-Myers Squibb Company, Research and Development, 350 Carter Road, Hopewell, NJ 08540 United States.
  • Corte JR; Bristol-Myers Squibb Company, Research and Development, 350 Carter Road, Hopewell, NJ 08540 United States.
  • Rossi KA; Bristol-Myers Squibb Company, Research and Development, 350 Carter Road, Hopewell, NJ 08540 United States.
  • Bozarth JM; Bristol-Myers Squibb Company, Research and Development, 311 Pennington-Rocky Hill Road, Pennington, NJ 08543-2130 United States.
  • Wu Y; Bristol-Myers Squibb Company, Research and Development, 311 Pennington-Rocky Hill Road, Pennington, NJ 08543-2130 United States.
  • Sheriff S; Bristol-Myers Squibb Company, Research and Development, US Rt. 206 & Province Line Road, Princeton, NJ 08540 United States.
  • Myers JE; Bristol-Myers Squibb Company, Research and Development, US Rt. 206 & Province Line Road, Princeton, NJ 08540 United States.
  • Luettgen JM; Bristol-Myers Squibb Company, Research and Development, 311 Pennington-Rocky Hill Road, Pennington, NJ 08543-2130 United States.
  • Seiffert DA; Bristol-Myers Squibb Company, Research and Development, US Rt. 206 & Province Line Road, Princeton, NJ 08540 United States.
  • Wexler RR; Bristol-Myers Squibb Company, Research and Development, 350 Carter Road, Hopewell, NJ 08540 United States.
  • Quan ML; Bristol-Myers Squibb Company, Research and Development, 350 Carter Road, Hopewell, NJ 08540 United States. Electronic address: mimi.quan@bms.com.
Bioorg Med Chem Lett ; 27(17): 4056-4060, 2017 09 01.
Article em En | MEDLINE | ID: mdl-28780160
ABSTRACT
A series of macrocyclic factor XIa (FXIa) inhibitors was designed based on an analysis of the crystal structures of the acyclic phenylimidazole compounds. Further optimization using structure-based design led to inhibitors with pM affinity for FXIa, excellent selectivity against a panel of relevant serine proteases, and good potency in the activated partial thromboplastin time (aPTT) clotting assay.
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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Fator XIa / Inibidores de Serina Proteinase / Compostos Macrocíclicos / Imidazóis Idioma: En Ano de publicação: 2017 Tipo de documento: Article
Texto completo
Imprimir
XML
PubMed Links
Buscar no Google

Texto completo: 1 Base de dados: MEDLINE Assunto principal: Fator XIa / Inibidores de Serina Proteinase / Compostos Macrocíclicos / Imidazóis Idioma: En Ano de publicação: 2017 Tipo de documento: Article