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Discovery of trifluoromethyl(pyrimidin-2-yl)azetidine-2-carboxamides as potent, orally bioavailable TGR5 (GPBAR1) agonists: structure-activity relationships, lead optimization, and chronic in vivo efficacy.
Phillips, Dean P; Gao, Wenqi; Yang, Yang; Zhang, Guobao; Lerario, Isabelle K; Lau, Thomas L; Jiang, Jiqing; Wang, Xia; Nguyen, Deborah G; Bhat, B Ganesh; Trotter, Carol; Sullivan, Heather; Welzel, Gustav; Landry, Jannine; Chen, Yali; Joseph, Sean B; Li, Chun; Gordon, W Perry; Richmond, Wendy; Johnson, Kevin; Bretz, Angela; Bursulaya, Badry; Pan, Shifeng; McNamara, Peter; Seidel, H Martin.
Affiliation
  • Phillips DP; Departments of †Medicinal Chemistry, ‡Drug Discovery Biology, §Pharmacology, ∥Pharmacokinetics, and ⊥Structural Biology, Genomics Institute of the Novartis Research Foundation , 10675 John Jay Hopkins Drive, San Diego, California 92121, United States.
J Med Chem ; 57(8): 3263-82, 2014 Apr 24.
Article in En | MEDLINE | ID: mdl-24666203
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Piperazines / Receptors, G-Protein-Coupled / Hypoglycemic Agents Limits: Animals / Humans / Male Language: En Journal: J Med Chem Journal subject: QUIMICA Year: 2014 Document type: Article Affiliation country: Country of publication:
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Piperazines / Receptors, G-Protein-Coupled / Hypoglycemic Agents Limits: Animals / Humans / Male Language: En Journal: J Med Chem Journal subject: QUIMICA Year: 2014 Document type: Article Affiliation country: Country of publication: