作者:Enrico Morera、Vincenzo Di Marzo、Ludovica Monti、Marco Allarà、Aniello Schiano Moriello、Marianna Nalli、Giorgio Ortar、Luciano De Petrocellis
DOI:10.1016/j.bmcl.2016.01.071
日期:2016.3
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.
制备了一系列基于药效团模型设计的31种芳基硼酸,用于各种TRPV1拮抗剂,并在FAAH和TRPV1通道上进行了测试。其中四个化合物,即化合物3c,4a,5a,b充当双重FAAH / TRPV1阻滞剂,IC 50值在0.56至8.11μM之间,而其他十种化合物(化合物1c,f – i,2c – f,4b)则抑制FAAH和激活/脱敏的TRPV1。