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3-Substituted 3-(4-aryloxyaryl)-propanoic acids as GPR40 agonists

Walsh, Shawn P ; Severino, Alexandra ; Zhou, Changyou ; He, Jiafang ; Liang, Gui-Bai ; Tan, Carina P ; Cao, Jin ; Eiermann, George J ; Xu, Ling ; Salituro, Gino ; Howard, Andrew D ; Mills, Sander G ; Yang, Lihu

Bioorganic & Medicinal Chemistry Letters, 2011, Vol.21(11), pp.3390-3394 [Peer Reviewed Journal]

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  • Title:
    3-Substituted 3-(4-aryloxyaryl)-propanoic acids as GPR40 agonists
  • Author: Walsh, Shawn P ; Severino, Alexandra ; Zhou, Changyou ; He, Jiafang ; Liang, Gui-Bai ; Tan, Carina P ; Cao, Jin ; Eiermann, George J ; Xu, Ling ; Salituro, Gino ; Howard, Andrew D ; Mills, Sander G ; Yang, Lihu
  • Description: The design, synthesis, and structure–activity relationship (SAR) for a series of β-substituted 3-(4-aryloxy)propanoic acid GPR40 agonists is described. Systematic replacement of the pendant aryloxy group led to identification of potent GPR40 agonists. In order to identify candidates suitable for in vivo validation of the target, serum shifted potency and pharmacokinetic properties were determined for several compounds. Finally, further profiling of compound is presented, including demonstration of enhanced glucose tolerance in an in vivo mouse model. The design, synthesis, and structure–activity relationship (SAR) for a series of β-substituted 3-(4-aryloxyaryl)propanoic acid GPR40 agonists is described. Systematic replacement of the pendant aryloxy group led to identification of potent GPR40 agonists. In order to identify candidates suitable for in vivo validation of the target, serum shifted potency and pharmacokinetic properties were determined for several compounds. Finally, further profiling of compound is presented, including demonstration of enhanced glucose tolerance in an in vivo mouse model.
  • Is Part Of: Bioorganic & Medicinal Chemistry Letters, 2011, Vol.21(11), pp.3390-3394
  • Identifier: ISSN: 0960-894X ; E-ISSN: 1464-3405 ; DOI: 10.1016/j.bmcl.2011.03.114
  • Subjects: Gpr40 ; Agonist ; 3-(4-Aryloxy)-Propanoic Acids ; Diabetic ; Gdis ; Medicine ; Chemistry ; Anatomy & Physiology
  • Language: English
  • Source: ScienceDirect Journals (Elsevier)

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