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Discovery of a novel trans-1,4-dioxycyclohexane GPR119 agonist series.
Han, Sangdon; Narayanan, Sanju; Kim, Sun Hee; Calderon, Imelda; Zhu, Xiuwen; Kawasaki, Andrew; Yue, Dawei; Lehmann, Juerg; Wong, Amy; Buzard, Daniel J; Semple, Graeme; Carroll, Chris; Chu, Zhi-Liang; Al-Sharmma, Hussein; Shu, Hsin-Hui; Tung, Shiu-Feng; Unett, David J; Behan, Dominic P; Yoon, Woo Hyun; Morgan, Michael; Usmani, Khawja A; Chen, Chuan; Sadeque, Abu; Leonard, James N; Jones, Robert M.
Afiliação
  • Han S; Arena Pharmaceuticals, 6154 Nancy Ridge Drive, San Diego, CA 92121, USA. Electronic address: shan@arenapharm.com.
  • Narayanan S; Arena Pharmaceuticals, 6154 Nancy Ridge Drive, San Diego, CA 92121, USA.
  • Kim SH; Arena Pharmaceuticals, 6154 Nancy Ridge Drive, San Diego, CA 92121, USA.
  • Calderon I; Arena Pharmaceuticals, 6154 Nancy Ridge Drive, San Diego, CA 92121, USA.
  • Zhu X; Arena Pharmaceuticals, 6154 Nancy Ridge Drive, San Diego, CA 92121, USA.
  • Kawasaki A; Arena Pharmaceuticals, 6154 Nancy Ridge Drive, San Diego, CA 92121, USA.
  • Yue D; Arena Pharmaceuticals, 6154 Nancy Ridge Drive, San Diego, CA 92121, USA.
  • Lehmann J; Arena Pharmaceuticals, 6154 Nancy Ridge Drive, San Diego, CA 92121, USA.
  • Wong A; Arena Pharmaceuticals, 6154 Nancy Ridge Drive, San Diego, CA 92121, USA.
  • Buzard DJ; Arena Pharmaceuticals, 6154 Nancy Ridge Drive, San Diego, CA 92121, USA.
  • Semple G; Arena Pharmaceuticals, 6154 Nancy Ridge Drive, San Diego, CA 92121, USA.
  • Carroll C; Arena Pharmaceuticals, 6154 Nancy Ridge Drive, San Diego, CA 92121, USA.
  • Chu ZL; Arena Pharmaceuticals, 6154 Nancy Ridge Drive, San Diego, CA 92121, USA.
  • Al-Sharmma H; Arena Pharmaceuticals, 6154 Nancy Ridge Drive, San Diego, CA 92121, USA.
  • Shu HH; Arena Pharmaceuticals, 6154 Nancy Ridge Drive, San Diego, CA 92121, USA.
  • Tung SF; Arena Pharmaceuticals, 6154 Nancy Ridge Drive, San Diego, CA 92121, USA.
  • Unett DJ; Arena Pharmaceuticals, 6154 Nancy Ridge Drive, San Diego, CA 92121, USA.
  • Behan DP; Arena Pharmaceuticals, 6154 Nancy Ridge Drive, San Diego, CA 92121, USA.
  • Yoon WH; Arena Pharmaceuticals, 6154 Nancy Ridge Drive, San Diego, CA 92121, USA.
  • Morgan M; Arena Pharmaceuticals, 6154 Nancy Ridge Drive, San Diego, CA 92121, USA.
  • Usmani KA; Arena Pharmaceuticals, 6154 Nancy Ridge Drive, San Diego, CA 92121, USA.
  • Chen C; Arena Pharmaceuticals, 6154 Nancy Ridge Drive, San Diego, CA 92121, USA.
  • Sadeque A; Arena Pharmaceuticals, 6154 Nancy Ridge Drive, San Diego, CA 92121, USA.
  • Leonard JN; Arena Pharmaceuticals, 6154 Nancy Ridge Drive, San Diego, CA 92121, USA.
  • Jones RM; Arena Pharmaceuticals, 6154 Nancy Ridge Drive, San Diego, CA 92121, USA.
Bioorg Med Chem Lett ; 25(15): 3034-8, 2015 Aug 01.
Article em En | MEDLINE | ID: mdl-26048791
ABSTRACT
The design and optimization of a novel trans-1,4-dioxycyclohexane GPR119 agonist series is described. A lead compound 21 was found to be a potent and efficacious GPR119 agonist across species, and possessed overall favorable pharmaceutical properties. Compound 21 demonstrated robust acute and chronic regulatory effects on glycemic parameters in the diabetic or non-diabetic rodent models.
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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Cicloexanos / Receptores Acoplados a Proteínas G / Diabetes Mellitus Tipo 2 / Hipoglicemiantes Limite: Animals / Humans / Male Idioma: En Ano de publicação: 2015 Tipo de documento: Article
Texto completo
Imprimir
XML
PubMed Links
Buscar no Google

Texto completo: 1 Base de dados: MEDLINE Assunto principal: Cicloexanos / Receptores Acoplados a Proteínas G / Diabetes Mellitus Tipo 2 / Hipoglicemiantes Limite: Animals / Humans / Male Idioma: En Ano de publicação: 2015 Tipo de documento: Article