Diaryl urea analogues of SB-334867 as orexin-1 receptor antagonists

DA Perrey, BP Gilmour, SP Runyon, BF Thomas…

Index: Perrey, David A.; Gilmour, Brian P.; Runyon, Scott P.; Thomas, Brian F.; Zhang, Yanan Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 10 p. 2980 - 2985

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Citation Number: 13

Abstract

Abstract As a part of our program to develop OX1–CB1 bivalent ligands, we required a better understanding of the basic structure–activity relationships (SARs) of orexin antagonists. A series of SB-334867 analogues were synthesized and evaluated in calcium mobilization assays. SAR results suggest that the 2-methylbenzoxazole moiety may be replaced with a disubstituted 4-aminophenyl group without loss of activity and an electron-deficient system ...