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Structure-activity relationships of 4-hydroxy-4-biaryl-proline acylsulfonamide tripeptides: A series of potent NS3 protease inhibitors for the treatment of hepatitis C virus.
Wang, Alan Xiangdong; Chen, Jie; Zhao, Qian; Sun, Li-Qiang; Friborg, Jacques; Yu, Fei; Hernandez, Dennis; Good, Andrew C; Klei, Herbert E; Rajamani, Ramkumar; Mosure, Kathy; Knipe, Jay O; Li, Danshi; Zhu, Jialong; Levesque, Paul C; McPhee, Fiona; Meanwell, Nicholas A; Scola, Paul M.
Afiliación
  • Wang AX; Department of Discovery Chemistry, Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492, United States. Electronic address: alan.wang@bms.com.
  • Chen J; Department of Discovery Chemistry, Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492, United States.
  • Zhao Q; Department of Discovery Chemistry, Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492, United States.
  • Sun LQ; Department of Discovery Chemistry, Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492, United States.
  • Friborg J; Department of Virology, Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492, United States.
  • Yu F; Department of Virology, Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492, United States.
  • Hernandez D; Department of Virology, Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492, United States.
  • Good AC; Department of Computational-Aided Drug Design, Bristol-Myers Squibb Research and Development, Research Parkway, Wallingford, CT 06492, United States.
  • Klei HE; Department of Computational-Aided Drug Design, Bristol-Myers Squibb Research and Development, Research Parkway, Wallingford, CT 06492, United States.
  • Rajamani R; Department of Computational-Aided Drug Design, Bristol-Myers Squibb Research and Development, Research Parkway, Wallingford, CT 06492, United States.
  • Mosure K; Global Clinical Research, Bristol-Myers Squibb Research and Development, 5, Research Parkway, Wallingford, CT 06492, United States.
  • Knipe JO; Global Clinical Research, Bristol-Myers Squibb Research and Development, 5, Research Parkway, Wallingford, CT 06492, United States.
  • Li D; Global Clinical Research, Bristol-Myers Squibb Research and Development, 5, Research Parkway, Wallingford, CT 06492, United States.
  • Zhu J; Global Clinical Research, Bristol-Myers Squibb Research and Development, 5, Research Parkway, Wallingford, CT 06492, United States.
  • Levesque PC; Global Clinical Research, Bristol-Myers Squibb Research and Development, 5, Research Parkway, Wallingford, CT 06492, United States.
  • McPhee F; Department of Virology, Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492, United States.
  • Meanwell NA; Department of Discovery Chemistry, Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492, United States.
  • Scola PM; Department of Discovery Chemistry, Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492, United States.
Bioorg Med Chem Lett ; 27(3): 590-596, 2017 02 01.
Article en En | MEDLINE | ID: mdl-28011221
ABSTRACT
The design and synthesis of a series of tripeptide acylsulfonamides as potent inhibitors of the HCV NS3/4A serine protease is described. These analogues house a C4 aryl, C4 hydroxy-proline at the S2 position of the tripeptide scaffold. Information relating to structure-activity relationships as well as the pharmacokinetic and cardiovascular profiles of these analogues is provided.
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Texto completo: 1 Base de datos: MEDLINE Asunto principal: Antivirales / Oligopéptidos / Inhibidores de Proteasas / Proteínas no Estructurales Virales / Hepacivirus Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2017 Tipo del documento: Article
Texto completo
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Texto completo: 1 Base de datos: MEDLINE Asunto principal: Antivirales / Oligopéptidos / Inhibidores de Proteasas / Proteínas no Estructurales Virales / Hepacivirus Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2017 Tipo del documento: Article