Title of article :
Design, synthesis, and SAR studies on a series of 2-pyridinylpiperazines as potent antagonists of the melanocortin-4 receptor
Author/Authors :
Joe A. Tran، نويسنده , , Joseph Pontillo، نويسنده , , Beth A. Fleck، نويسنده , , Dragan Marinkovic، نويسنده , , Melissa Arellano، نويسنده , , Fabio C. Tucci، نويسنده , , Marion Lanier، نويسنده , , John Saunders، نويسنده , , Wanlong Jiang، نويسنده , , Caroline W. Chen، نويسنده , , Alan C. Foster، نويسنده , , Chen Chen، نويسنده ,
Abstract :
A series of 2-pyridinylpiperazines derived from β-Ala-(2,4-Cl)Phe dipeptide was synthesized for the study of their SARs and possible interactions with the MC4 receptor. Compounds such as 11k (Ki = 6.5 nM) possessed high potency.
Keywords :
melanocortin , Antagonist , 2-Pyridinylpiperazine , synthesis
