Author/Authors :
Bo Liu، نويسنده , , Gang Liu، نويسنده , , Zhili Xin، نويسنده , , Micheal D. Serby، نويسنده , , Baolin Wu&Hongyu Zhao، نويسنده , , Verlyn G. Schaefer، نويسنده , , H. Douglas Falls، نويسنده , , Wiweka Kaszubska، نويسنده , , Christine A.Collins، نويسنده , , Hing L. Sham، نويسنده ,
Abstract :
Novel isoxazole carboxamides have been identified as growth hormone secretagogue receptor (GHS-R) antagonists. Substituent modification off the 5-position of the isoxazole ring led to analogues with potent binding affinity and functional antagonism of GHS-R. A potent analogue (32) with high aqueous solubility and good GPCR selectivity was also identified as a potential pharmacological tool for in vivo studies.
