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• W2772468450 startingPage "429" @default.
• W2772468450 abstract "GPR40 partial agonism is a promising new mechanism for the treatment of type 2 diabetes mellitus with clinical proof of concept. Most of the GPR40 agonists in the literature have a carboxylic acid functional group, which may pose a risk for idiosyncratic drug toxicity. A novel series of GPR40 agonists containing a tetrazole as a carboxylic acid bioisostere was identified. This series of compounds features a benzo[b]thiophene as the center ring, which is prone to oxidation during phase 1 metabolism. Following SAR optimization targeting GPR40 agonist activity and intrinsic clearance in microsomes (human and rat), potent and metabolically stable compounds were selected for in vivo evaluation. The compounds are efficacious at lowering blood glucose in a SD rat oGTT model." @default.
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• W2772468450 date "2018-02-01" @default.
• W2772468450 modified "2023-10-16" @default.
• W2772468450 title "Discovery of novel benzo[b]thiophene tetrazoles as non-carboxylate GPR40 agonists" @default.
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• W2772468450 doi "https://doi.org/10.1016/j.bmcl.2017.12.022" @default.
• W2772468450 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/29258772" @default.
• W2772468450 hasPublicationYear "2018" @default.
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