Sulfonyl fluoride inhibitors of fatty acid amide hydrolase

SO Alapafuja, SP Nikas, IT Bharathan…

Index: Alapafuja, Shakiru O.; Nikas, Spyros P.; Bharathan, Indu T.; Shukla, Vidyanand G.; Nasr, Mahmoud L.; Bowman, Anna L.; Zvonok, Nikolai; Li, Jing; Shi, Xiaomeng; Engen, John R.; Makriyannis, Alexandros Journal of Medicinal Chemistry, 2012 , vol. 55, # 22 p. 10074 - 10089

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Citation Number: 16

Abstract

Sulfonyl fluorides are known to inhibit esterases. Early work from our laboratory has identified hexadecyl sulfonylfluoride (AM374) as a potent in vitro and in vivo inhibitor of fatty acid amide hydrolase (FAAH). We now report on later generation sulfonyl fluoride analogs that exhibit potent and selective inhibition of FAAH. Using recombinant rat and human FAAH, we show that 5-(4-hydroxyphenyl) pentanesulfonyl fluoride (AM3506) has similar ...