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  • Title: Synthesis and SAR of 1,2,3,4-tetrahydroisoquinolin-1-ones as novel G-protein-coupled receptor 40 (GPR40) antagonists.
    Author: Humphries PS, Benbow JW, Bonin PD, Boyer D, Doran SD, Frisbie RK, Piotrowski DW, Balan G, Bechle BM, Conn EL, Dirico KJ, Oliver RM, Soeller WC, Southers JA, Yang X.
    Journal: Bioorg Med Chem Lett; 2009 May 01; 19(9):2400-3. PubMed ID: 19346127.
    Abstract:
    The development of a series of novel 1,2,3,4-tetrahydroisoquinolin-1-ones as antagonists of G protein-coupled receptor 40 (GPR40) is described. The synthesis, in vitro inhibitory values for GPR40, in vitro microsomal clearance and rat in vivo clearance data are discussed. Initial hits displayed high rat in vivo clearances that were higher than liver blood flow. Optimization of rat in vivo clearance was achieved and led to the identification of 15i, whose rat oral pharmacokinetic data is reported.
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