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  • Title: Synthesis and SAR of heterocyclic carboxylic acid isosteres based on 2-biarylethylimidazole as bombesin receptor subtype-3 (BRS-3) agonists for the treatment of obesity.
    Author: Hadden M, Goodman A, Guo C, Guzzo PR, Henderson AJ, Pattamana K, Ruenz M, Sargent BJ, Swenson B, Yet L, Liu J, He S, Sebhat IK, Lin LS, Tamvakopoulos C, Peng Q, Kan Y, Palyha O, Kelly TM, Guan XM, Metzger JM, Reitman ML, Nargund RP.
    Journal: Bioorg Med Chem Lett; 2010 May 01; 20(9):2912-5. PubMed ID: 20347296.
    Abstract:
    SAR around non-peptidic potent bombesin receptor subtype-3 (BRS-3) agonist lead 2 is presented. Attempts to replace the carboxylic acid with heterocyclic isosteres to improve oral bioavailability and brain penetration are described.
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