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Bioorg Med Chem Lett
; 14(20): 5223-6, 2004 Oct 18.
Article
in English
| MEDLINE
| ID: mdl-15380232
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.