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.

Butini, S., Gemma, S., Brindisi, M., Maramai, S., Minetti, P., Celona, D., et al. (2013). Identification of a novel arylpiperazine scaffold for fatty acid amide hydrolase inhibition with improved drug disposition properties. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 23(2), 492-495 [10.1016/j.bmcl.2012.11.035].

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

FEZZA, FILOMENA;
2013-01-01

Abstract

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.
gen-2013
Pubblicato
Rilevanza internazionale
Articolo
Esperti anonimi
Settore BIO/10 - BIOCHIMICA
English
Con Impact Factor ISI
Butini, S., Gemma, S., Brindisi, M., Maramai, S., Minetti, P., Celona, D., et al. (2013). Identification of a novel arylpiperazine scaffold for fatty acid amide hydrolase inhibition with improved drug disposition properties. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 23(2), 492-495 [10.1016/j.bmcl.2012.11.035].
Butini, S; Gemma, S; Brindisi, M; Maramai, S; Minetti, P; Celona, D; Napolitano, R; Borsini, F; Cabri, W; Fezza, F; Merlini, L; Dallavalle, S; Campian...espandi
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/2108/79189
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