Discovery and pharmacological evaluation of growth hormone secretagogue receptor antagonists

…, HD Falls, CW Lin, CA Ogiela, CA Collins…

Index: Zhao, Hongyu; Xin, Zhili; Liu, Gang; Schaefer, Verlyn G.; Falls, H. Douglas; Kaszubska, Wiweka; Collins, Christine A.; Sham, Hing L. Journal of Medicinal Chemistry, 2004 , vol. 47, # 27 p. 6655 - 6657

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Citation Number: 37

Abstract

The discovery and pharmacological evaluation of potent, selective, and orally bioavailable growth hormone secretagogue receptor (GHS-R) antagonists are reported. Previously, 2, 4- diaminopyrimidine-based GHS-R antagonists reported from our laboratories have been shown to be dihydrofolate reductase (DHFR) inhibitors. By comparing the X-ray crystal structure of DHFR docked with our GHS-R antagonists and GHS-R modeling, we ...