Title of article :
Design and synthesis of potent and selective 1,3,4-trisubstituted-2-oxopiperazine based melanocortin-4 receptor agonists
Author/Authors :
Xinrong Tian، نويسنده , , Rajesh K. Mishra، نويسنده , , Adrian G. Switzer، نويسنده , , X. Eric Hu، نويسنده , , Nick Kim، نويسنده , , Adam W. Mazur، نويسنده , , Frank H. Ebetino، نويسنده , , John A. Wos، نويسنده , , Doreen Crossdoersen، نويسنده , , Beth B. Pinney، نويسنده , , Julie A. Farmer، نويسنده , , Russell J. Sheldon، نويسنده ,
Abstract :
The design and synthesis of a series of potent 1,3,4-trisubstituted-2-oxopiperazine based MC4 agonists are described. The tripeptidomimetic analogs (12a,b and 23) and the dipeptidomimetic 27 displayed single-nanomolar binding affinity and agonist potency for MC4R and excellent selectivity for MC4R relative to MC1R.
Keywords :
2-Oxopiperazine , peptidomimetics , Melanocortin-4 , Agonists
