Design, synthesis and biological evaluation of potent FAAH inhibitors

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• 作者：Wei Tuo ; Natascha Leleu-Chavain ; Amé ; lie Barczyk ; Nicolas Renault ; Lucas Lemaire ; Philippe Chavatte ; Ré ; gis Millet ; ^{regis.millet@univ-lille2.fr" class="auth_mail" title="E-mail the corresponding author}
• 关键词：FAAH inhibitor ; AEA ; PEA ; Cannabinoid receptors ; PPAR-α
• 刊名：Bioorganic & Medicinal Chemistry Letters
• 出版年：2016
• 出版时间：1 June 2016
• 年：2016
• 卷：26
• 期：11
• 页码：2701-2705
• 全文大小：559 K

文摘

A new series of 3-carboxamido-5-aryl-isoxazoles was designed, synthesized and evaluated for their biological activity. Different pharmacomodulations have been explored and the lipophilicity of these compounds was assessed. Investigation of the in vitro biological activity led to the identification of 5 compounds as potent FAAH inhibitors, their good FAAH inhibition capacity is probably correlated with their suitable lipophilicity. Specifically, compound 25 showed similar inhibition potency against FAAH in comparison with URB597, one of the most potent FAAH inhibitor known to date.