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. © 2012 Elsevier Ltd. All rights reserved.
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
Butini, Stefania;Gemma, Sandra;Maramai, Samuele;Campiani, Giuseppe;
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. © 2012 Elsevier Ltd. All rights reserved.
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https://hdl.handle.net/11365/43475
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