J. Pontillo, Dragan Marinkovic, Joe A. Tran
Oct 15, 2005
Citations
1
Influential Citations
8
Citations
Journal
Bioorganic & medicinal chemistry letters
Abstract
Piperazinebenzylamines bearing a small N-(1-methoxy-2-propyl) side chain were found to be potent and selective antagonists of the human melanocortin-4 (MC4) receptor. Compound 7b, having K(i) values of 6.9 and 2800 nM at the human MC4 and MC3 receptors, respectively, has moderate oral bioavailability in mice, which is improved relative to the arylethyl analogues.