Novel isoxazole carboxamides as growth hormone secretagogue receptor (GHS-R) antagonists

…, H Zhao, VG Schaefer, HD Falls, W Kaszubska…

Index: Liu, Bo; Liu, Gang; Xin, Zhili; Serby, Micheal D.; Zhao, Hongyu; Schaefer, Verlyn G.; Falls, H. Douglas; Kaszubska, Wiweka; Collins, Christine A.; Sham, Hing L. Bioorganic and Medicinal Chemistry Letters, 2004 , vol. 14, # 20 p. 5223 - 5226

Full Text: HTML

Citation Number: 28

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.