| 17964151 |
Chen CW, Tran JA, Fleck BA, Tucci FC, Jiang W, Chen C: Synthesis and characterization of trans-4-(4-chlorophenyl) pyrrolidine-3-carboxamides of piperazinecyclohexanes as ligands for the melanocortin-4 receptor. Bioorg Med Chem Lett. 2007 Dec 15;17(24):6825-31. Epub 2007 Oct 17.
A series of trans-N-alkyl-4-(4-chlorophenyl) pyrrolidine-3-carboxamides of piperazinecyclohexanemethylamines was synthesized and characterized for binding and function at the melanocortin-4 receptor (MC4R), and several potent benzylamine derivatives were identified. Compound 18 v was found to bind MC4R with potent affinity (K (i)=0.5 nM) and high selectivity over the other melanocortin subtypes and behaved as a functional antagonist (IC (50)=48 nM). |
3(0,0,0,3) |