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Discovery of the oxazabicyclo[3.3.1]nonane derivatives as potent and orally active GPR119 agonists.
Dai, Xing; Stamford, Andrew; Liu, Hong; Neustadt, Bernard; Hao, Jingsong; Kowalski, Tim; Hawes, Brian; Xu, Xiaoying; Baker, Hana; O'Neill, Kim; Woods, Morgan; Tang, Huadong; Greenlee, William.
Afiliación
  • Dai X; Department of Medicinal Chemistry, Merck Research Laboratory, 2015 Galloping Hill Road, Kenilworth, NJ 07033, United States.
  • Stamford A; Department of Medicinal Chemistry, Merck Research Laboratory, 2015 Galloping Hill Road, Kenilworth, NJ 07033, United States.
  • Liu H; Department of Medicinal Chemistry, Merck Research Laboratory, 2015 Galloping Hill Road, Kenilworth, NJ 07033, United States.
  • Neustadt B; Department of Medicinal Chemistry, Merck Research Laboratory, 2015 Galloping Hill Road, Kenilworth, NJ 07033, United States.
  • Hao J; Department of Medicinal Chemistry, Merck Research Laboratory, 2015 Galloping Hill Road, Kenilworth, NJ 07033, United States.
  • Kowalski T; Department of Biology, Merck Research Laboratory, 2015 Galloping Hill Road, Kenilworth, NJ 07033, United States.
  • Hawes B; Department of Biology, Merck Research Laboratory, 2015 Galloping Hill Road, Kenilworth, NJ 07033, United States.
  • Xu X; Department of Drug Metabolism, Merck Research Laboratory, 2015 Galloping Hill Road, Kenilworth, NJ 07033, United States.
  • Baker H; Department of Biology, Merck Research Laboratory, 2015 Galloping Hill Road, Kenilworth, NJ 07033, United States.
  • O'Neill K; Department of Biology, Merck Research Laboratory, 2015 Galloping Hill Road, Kenilworth, NJ 07033, United States.
  • Woods M; Department of Biology, Merck Research Laboratory, 2015 Galloping Hill Road, Kenilworth, NJ 07033, United States.
  • Tang H; Department of Drug Metabolism, Merck Research Laboratory, 2015 Galloping Hill Road, Kenilworth, NJ 07033, United States.
  • Greenlee W; Department of Medicinal Chemistry, Merck Research Laboratory, 2015 Galloping Hill Road, Kenilworth, NJ 07033, United States.
Bioorg Med Chem Lett ; 25(22): 5291-4, 2015 Nov 15.
Article en En | MEDLINE | ID: mdl-26433449
ABSTRACT
The design and synthesis of two conformationally restricted oxazabicyclo octane derivatives as GRP119 agonists is described. Derivatives of scaffold C, with syn configuration, have the best overall profiles with respect to solubility and in vivo efficacy. Compound 25a was found to have extremely potent agonistic activity and was orally active in lowering blood glucose levels in a mouse oral glucose tolerance test at a dose of 0.1 mg/kg.
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Texto completo: 1 Bases de datos: MEDLINE Asunto principal: Pirimidinas / Receptores Acoplados a Proteínas G / Compuestos de Azabiciclo / Hipoglucemiantes Límite: Animals / Humans Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2015 Tipo del documento: Article País de afiliación: Estados Unidos
Texto completo
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Texto completo: 1 Bases de datos: MEDLINE Asunto principal: Pirimidinas / Receptores Acoplados a Proteínas G / Compuestos de Azabiciclo / Hipoglucemiantes Límite: Animals / Humans Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2015 Tipo del documento: Article País de afiliación: Estados Unidos