We herein describe the systematic approach used to develop new analogs of compd. 2 (I), 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 derivs. 4b and 5c as potent, reversible and noncompetitive FAAH inhibitors.
Stefania Butini, Sandra Gemma, Margherita Brindisi, Samuele Maramai Patrizia Minetti, Diana Celona, Raffaella Napolitano Franco Borsini, 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
Walter Cabri;
2013
Abstract
We herein describe the systematic approach used to develop new analogs of compd. 2 (I), 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 derivs. 4b and 5c as potent, reversible and noncompetitive FAAH inhibitors.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
