Synthesis and evaluation of benzothiazole-based analogues as novel, potent, and selective fatty acid amide hydrolase inhibitors

…, D Zhang, SP Brown, T Kolasa, C Surowy…

Index: Wang, Xueqing; Sarris, Katerina; Kage, Karen; Zhang, Di; Brown, Scott P.; Kolasa, Teodozyi; Surowy, Carol; El Kouhen, Odile F.; Muchmore, Steven W.; Brioni, Jorge D.; Stewart, Andrew O. Journal of Medicinal Chemistry, 2009 , vol. 52, # 1 p. 170 - 180

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Citation Number: 97

Abstract

High-throughput screening (HTS) identified benzothiazole analogue 3 as a potent fatty acid amide hydrolase (FAAH) inhibitor. Structure− activity relationship (SAR) studies indicated that the sulfonyl group, the piperidine ring and benzothiazole were the key components to their activity, with 16j being the most potent analogue in this series. Time-dependent preincubation study of compound 3 was consistent with it being a reversible inhibitor. ...