Author/Authors :
Wanlong Jiang، نويسنده , , Fabio C. Tucci، نويسنده , , Caroline W. Chen، نويسنده , , Melissa Arellano، نويسنده , , Joe A. Tran، نويسنده , , Nicole S. White، نويسنده , , Dragan Marinkovic، نويسنده , , Joseph Pontillo، نويسنده , , Beth A. Fleck، نويسنده , , Jenny Wen، نويسنده , , John Saunders، نويسنده , , Ajay Madan، نويسنده , , Alan C. Foster، نويسنده , , Chen Chen، نويسنده ,
Abstract :
A series of 3-arylpropionylpiperazines were synthesized as antagonists of the melanocortin-4 receptor. Their potency was found to be increased by replacing the α-methyl substituent of the initial lead 11 with a larger s-Bu or i-Bu group. Further potency enhancement was observed when a glycine or β-alanine was incorporated onto the benzylamine. Some compounds demonstrated good potency, moderate selectivity, and oral bioavailability.
Keywords :
synthesis , Arylpropinylpiperazine , melanocortin , Antagonist
