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.
Identification of a novel arylpiperazine scaffold for fatty acid amide hydrolase inhibition with improved drug disposition properties / S. Butini, S. Gemma, M. Brindisi, S. Maramai, P. Minetti, D. Celona, R. Napolitano, F. Fezza, L. Merlini, S. Dallavalle, G. Campiani, M. Maccarrone. - In: BIOORGANIC & MEDICINAL CHEMISTRY LETTERS. - ISSN 0960-894X. - 23:2(2013 Jan 15), pp. 492-495.
Titolo: | Identification of a novel arylpiperazine scaffold for fatty acid amide hydrolase inhibition with improved drug disposition properties |
Autori: | |
Parole Chiave: | Fatty acid amide hydrolase (FAAH) ; Enzyme inhibitors ; Solubility ; Cannabinoid system ; Drug disposition properties |
Settore Scientifico Disciplinare: | Settore CHIM/06 - Chimica Organica |
Data di pubblicazione: | 15-gen-2013 |
Rivista: | |
Tipologia: | Article (author) |
Data ahead of print / Data di stampa: | 22-nov-2012 |
Digital Object Identifier (DOI): | http://dx.doi.org/10.1016/j.bmcl.2012.11.035 |
Appare nelle tipologie: | 01 - Articolo su periodico |
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