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Optimization of Pharmacokinetics through Manipulation of Physicochemical Properties in a Series of HCV Inhibitors.
Lazerwith, Scott E; Bahador, Gina; Canales, Eda; Cheng, Guofeng; Chong, Lee; Clarke, Michael O; Doerffler, Edward; Eisenberg, Eugene J; Hayes, Jaclyn; Lu, Bing; Liu, Qi; Matles, Mike; Mertzman, Michael; Mitchell, Michael L; Morganelli, Philip; Murray, Bernard P; Robinson, Margaret; Strickley, Robert G; Tessler, Megan; Tirunagari, Neeraj; Wang, Jianhong; Wang, Yujin; Zhang, Jennifer R; Zheng, Xubin; Zhong, Weidong; Watkins, William J.
Afiliação
  • Lazerwith SE; Medicinal Chemistry, Drug Metabolism, Biology, and Formulation and Process Development, Gilead Sciences, Inc. , 333 Lakeside Drive, Foster City, California 94404, United States.
  • Bahador G; Medicinal Chemistry, Drug Metabolism, Biology, and Formulation and Process Development, Gilead Sciences, Inc. , 333 Lakeside Drive, Foster City, California 94404, United States.
  • Canales E; Medicinal Chemistry, Drug Metabolism, Biology, and Formulation and Process Development, Gilead Sciences, Inc. , 333 Lakeside Drive, Foster City, California 94404, United States.
  • Cheng G; Medicinal Chemistry, Drug Metabolism, Biology, and Formulation and Process Development, Gilead Sciences, Inc. , 333 Lakeside Drive, Foster City, California 94404, United States.
  • Chong L; Medicinal Chemistry, Drug Metabolism, Biology, and Formulation and Process Development, Gilead Sciences, Inc. , 333 Lakeside Drive, Foster City, California 94404, United States.
  • Clarke MO; Medicinal Chemistry, Drug Metabolism, Biology, and Formulation and Process Development, Gilead Sciences, Inc. , 333 Lakeside Drive, Foster City, California 94404, United States.
  • Doerffler E; Medicinal Chemistry, Drug Metabolism, Biology, and Formulation and Process Development, Gilead Sciences, Inc. , 333 Lakeside Drive, Foster City, California 94404, United States.
  • Eisenberg EJ; Medicinal Chemistry, Drug Metabolism, Biology, and Formulation and Process Development, Gilead Sciences, Inc. , 333 Lakeside Drive, Foster City, California 94404, United States.
  • Hayes J; Medicinal Chemistry, Drug Metabolism, Biology, and Formulation and Process Development, Gilead Sciences, Inc. , 333 Lakeside Drive, Foster City, California 94404, United States.
  • Lu B; Medicinal Chemistry, Drug Metabolism, Biology, and Formulation and Process Development, Gilead Sciences, Inc. , 333 Lakeside Drive, Foster City, California 94404, United States.
  • Liu Q; Medicinal Chemistry, Drug Metabolism, Biology, and Formulation and Process Development, Gilead Sciences, Inc. , 333 Lakeside Drive, Foster City, California 94404, United States.
  • Matles M; Medicinal Chemistry, Drug Metabolism, Biology, and Formulation and Process Development, Gilead Sciences, Inc. , 333 Lakeside Drive, Foster City, California 94404, United States.
  • Mertzman M; Medicinal Chemistry, Drug Metabolism, Biology, and Formulation and Process Development, Gilead Sciences, Inc. , 333 Lakeside Drive, Foster City, California 94404, United States.
  • Mitchell ML; Medicinal Chemistry, Drug Metabolism, Biology, and Formulation and Process Development, Gilead Sciences, Inc. , 333 Lakeside Drive, Foster City, California 94404, United States.
  • Morganelli P; Medicinal Chemistry, Drug Metabolism, Biology, and Formulation and Process Development, Gilead Sciences, Inc. , 333 Lakeside Drive, Foster City, California 94404, United States.
  • Murray BP; Medicinal Chemistry, Drug Metabolism, Biology, and Formulation and Process Development, Gilead Sciences, Inc. , 333 Lakeside Drive, Foster City, California 94404, United States.
  • Robinson M; Medicinal Chemistry, Drug Metabolism, Biology, and Formulation and Process Development, Gilead Sciences, Inc. , 333 Lakeside Drive, Foster City, California 94404, United States.
  • Strickley RG; Medicinal Chemistry, Drug Metabolism, Biology, and Formulation and Process Development, Gilead Sciences, Inc. , 333 Lakeside Drive, Foster City, California 94404, United States.
  • Tessler M; Medicinal Chemistry, Drug Metabolism, Biology, and Formulation and Process Development, Gilead Sciences, Inc. , 333 Lakeside Drive, Foster City, California 94404, United States.
  • Tirunagari N; Medicinal Chemistry, Drug Metabolism, Biology, and Formulation and Process Development, Gilead Sciences, Inc. , 333 Lakeside Drive, Foster City, California 94404, United States.
  • Wang J; Medicinal Chemistry, Drug Metabolism, Biology, and Formulation and Process Development, Gilead Sciences, Inc. , 333 Lakeside Drive, Foster City, California 94404, United States.
  • Wang Y; Medicinal Chemistry, Drug Metabolism, Biology, and Formulation and Process Development, Gilead Sciences, Inc. , 333 Lakeside Drive, Foster City, California 94404, United States.
  • Zhang JR; Medicinal Chemistry, Drug Metabolism, Biology, and Formulation and Process Development, Gilead Sciences, Inc. , 333 Lakeside Drive, Foster City, California 94404, United States.
  • Zheng X; Medicinal Chemistry, Drug Metabolism, Biology, and Formulation and Process Development, Gilead Sciences, Inc. , 333 Lakeside Drive, Foster City, California 94404, United States.
  • Zhong W; Medicinal Chemistry, Drug Metabolism, Biology, and Formulation and Process Development, Gilead Sciences, Inc. , 333 Lakeside Drive, Foster City, California 94404, United States.
  • Watkins WJ; Medicinal Chemistry, Drug Metabolism, Biology, and Formulation and Process Development, Gilead Sciences, Inc. , 333 Lakeside Drive, Foster City, California 94404, United States.
ACS Med Chem Lett ; 2(10): 715-9, 2011 Oct 13.
Article em En | MEDLINE | ID: mdl-24900257
ABSTRACT
A novel series of HCV replication inhibitors based on a pyrido[3,2-d]pyrimidine core were optimized for pharmacokinetics (PK) in rats. Several associations between physicochemical properties and PK were identified and exploited to guide the design of compounds. In addition, a simple new metric that may aid in the prediction of bioavailability for compounds with higher polar surface area is described (3*HBD-cLogP).
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Texto completo: 1 Base de dados: MEDLINE Idioma: En Ano de publicação: 2011 Tipo de documento: Article
Texto completo
Imprimir
XML
PubMed Links
Buscar no Google

Texto completo: 1 Base de dados: MEDLINE Idioma: En Ano de publicação: 2011 Tipo de documento: Article