Author/Authors :
Andrew J. Souers، نويسنده , , Qi-Ju Gao، نويسنده , , Dariusz Wodka، نويسنده , , Andrew S. Judd، نويسنده , , Mathew M. Mulhern، نويسنده , , James J. Napier، نويسنده , , Michael E. Brune، نويسنده , , Eugene N. Bush، نويسنده , , Sevan J. Brodjian، نويسنده , , Brian D. Dayton، نويسنده , , Robin Shapiro، نويسنده , , Lisa E. Hernandez، نويسنده , , Kennan C. Marsh، نويسنده , , Hing L. Sham، نويسنده , , Christine A. Collins، نويسنده , , Philip R. Kym، نويسنده ,
Abstract :
A series of urea-based N-1-(2-aminoethyl)-indazoles was synthesized and evaluated for melanin-concentrating hormone receptor 1 (MCHr1) antagonism in both binding and functional assays. Several compounds that acted as MCHr1 antagonists were identified, and optimization afforded a compound with excellent binding affinity, good functional potency, and oral efficacy in a chronic model for weight loss in diet-induced obese mice.
