Arylboronic acids as dual-action FAAH and TRPV1 ligands

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• 作者：Enrico Morera^a ; ^{enrico.morera@uniroma1.it" class="auth_mail" title="E-mail the corresponding author} ; Vincenzo Di Marzo^b ; Ludovica Monti^a ; Marco Allarà ; ^b ; Aniello Schiano Moriello^b ; Marianna Nalli^a ; Giorgio Ortar^a ; Luciano De Petrocellis^b ; ^{luciano.depetrocellis@icb.cnr.it" class="auth_mail" title="E-mail the corresponding author}
• 关键词：Fatty acid amide hydrolase ; FAAH ; Transient receptor potential vanilloid type-1 channel ; TRPV1 ; Dual-ligands ; Boronic acids
• 刊名：Bioorganic & Medicinal Chemistry Letters
• 出版年：2016
• 出版时间：1 March 2016
• 年：2016
• 卷：26
• 期：5
• 页码：1401-1405
• 全文大小：1470 K

文摘

A series of 31 arylboronic acids designed on the basis of the pharmacophore model for a variety of TRPV1 antagonists was prepared and tested on FAAH and TRPV1 channel. Four of them, that is, compounds 3c, 4a, 5a,b acted as dual FAAH/TRPV1 blockers with IC₅₀ values between 0.56 and 8.11 μM whereas ten others (compounds 1c,f–i, 2c–f, 4b) inhibited FAAH and activated/desensitized TRPV1.