Author/Authors :
Joseph Pontillo، نويسنده , , Dragan Marinkovic، نويسنده , , Joe A. Tran، نويسنده , , Melissa Arellano، نويسنده , , Beth A. Fleck، نويسنده , , Jenny Wen، نويسنده , , Fabio C. Tucci، نويسنده , , Jodie Nelson، نويسنده , , John Saunders، نويسنده , , Alan C. Foster، نويسنده , , Chen Chen، نويسنده ,
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 Ki 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.
Keywords :
Melanocortin-4 , Piperazinebenzylamine , Antagonist , synthesis
