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ID: ALA1141935

Journal: Bioorg Med Chem Lett

Title: Aminopiperidine indazoles as orally efficacious melanin concentrating hormone receptor-1 antagonists.

Authors: Vasudevan A, Souers AJ, Freeman JC, Verzal MK, Gao J, Mulhern MM, Wodka D, Lynch JK, Engstrom KM, Wagaw SH, Brodjian S, Dayton B, Falls DH, Bush E, Brune M, Shapiro RD, Marsh KC, Hernandez LE, Collins CA, Kym PR.

Abstract: The synthesis and biological evaluation of novel 3-amino indazole melanin concentrating hormone receptor-1 antagonists are reported, several of which demonstrated functional activity of less than 100nM. Compounds 19 and 28, two of the more potent compounds identified in this study, were characterized by high exposure in the brain and demonstrated robust efficacy when dosed in diet-induced obese mice.

CiteXplore: 16203136

DOI: 10.1016/j.bmcl.2005.08.049