Identification of a novel arylpiperazine scaffold for fatty acid amide hydrolase inhibition with improved drug disposition properties

Butini, S; Gemma, S; Brindisi, M; Maramai, S; Minetti, P; Celona, D; Napolitano, R; Borsini, F; Cabri, W; Fezza, F; Merlini, L; Dallavalle, S; Campiani, G; Maccarrone, M

doi:10.1016/j.bmcl.2012.11.035

We herein describe the systematic approach used to develop new analogues of compound 2, recently identified as a potent and selective fatty acid amide hydrolase (FAAH) inhibitor. Aiming at identifying new scaffolds endowed with improved drug disposition properties with respect to the phenylpyrrole-based lead, we subjected it to two different structural modification strategies. This process allowed the identification of derivatives 4b and 5c as potent, reversible and non-competitive FAAH inhibitors. (C) 2012 Published by Elsevier Ltd.

Titolo:	Identification of a novel arylpiperazine scaffold for fatty acid amide hydrolase inhibition with improved drug disposition properties
Autori:	Butini S Gemma S Brindisi M Maramai S Minetti P Celona D Napolitano R Borsini F Cabri W Fezza F Merlini L Dallavalle S Campiani G MACCARRONE, Mauro mostra contributor esterni nascondi contributor esterni
Data di pubblicazione:	2013
Handle:	http://hdl.handle.net/11697/156046
Appare nelle tipologie:	1.1 Articolo in rivista

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