Author/Authors :
Joseph Pontillo، نويسنده , , Joseph A. Tran، نويسنده , , Melissa Arellano، نويسنده , , Beth A. Fleck، نويسنده , , Rajesh Huntley، نويسنده , , Dragan Marinkovic، نويسنده , , Marion Lanier، نويسنده , , Jodie Nelson، نويسنده , , Jessica Parker، نويسنده , , John Saunders، نويسنده , , Fabio C. Tucci، نويسنده , , Wanlong Jiang، نويسنده , , Caroline W. Chen، نويسنده , , Nicole S. White، نويسنده , , Alan C. Foster، نويسنده , , Chen Chen، نويسنده ,
Abstract :
SAR studies on a series of piperazinebenzenes directed toward the human melanocortin-4 receptor resulted in potent MC4R agonists. Replacement of the triazole moiety of an initial lead 4 by a basic nitrogen baring a lipophilic side-chain increased the binding affinities of these compounds. Analogs bearing an additional hetero-atom in the side-chain possessed good agonist potency. Thus, 11h had a Ki of 11 nM, and 13g exhibited an EC50 of 3.8 nM and a Ki of 6.4 nM.
Keywords :
melanocortin , MC4R , fax: +1-858-658-7619 , e-mail: cchen@neurocrine.com , Agonist.* Corresponding author. Tel.: +1-858-658-7630
