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ID: ALA1157884
Journal: Bioorg Med Chem Lett
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.
Authors: 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.
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.
CiteXplore: 20347296