Discovery of potent inhibitors of human and mouse fatty acid amide hydrolases

S Butini, M Brindisi, S Gemma, P Minetti…

Index: Butini, Stefania; Brindisi, Margherita; Gemma, Sandra; Minetti, Patrizia; Cabri, Walter; Gallo, Grazia; Vincenti, Silvia; Talamonti, Emanuela; Borsini, Franco; Caprioli, Antonio; Stasi, Maria Antonietta; Di Serio, Stefano; Ros, Sindu; Borrelli, Giuseppe; Maramai, Samuele; Fezza, Filomena; Campiani, Giuseppe; MacCarrone, Mauro Journal of Medicinal Chemistry, 2012 , vol. 55, # 15 p. 6898 - 6915

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Citation Number: 16

Abstract

Fatty acid amide hydrolase (FAAH, EC 3.5. 1.99) is the main enzyme catabolizing endocannabinoid fatty acid amides. FAAH inactivation promotes beneficial effects upon pain and anxiety without the side effects accompanying agonists of type-1 cannabinoid receptors. Aiming at discovering new selective FAAH inhibitors, we developed a series of compounds (5a–u) characterized by a functionalized heteroaromatic scaffold. Particularly, 5c and 5d ...