Design,synthesis and activity evaluation of benzamides as sEH inhibitors
In order to discover new anti-inflammatory compounds and improve the metabolic stability and solubility of A34 with good inhibitory activities on sEH,seven compounds(X-1-X-7)were designed and synthesized using compound A34 as the lead compound.The structures of the target compounds were confirmed by MS and 1H-NMR.With A34 as the positive control drug,all the target compounds were evaluated in vitro for inhibitory by Cayman fluorescence method.The results showed that most of target compounds showed varying degrees of inhibitory activities on sEH.Compound X-4 exhibited better inhibitory activity with IC50 value*of 0.1 nmol·L-1 compared with the positive control drug,and it could be developed for further research.
sEH inhibitorbenzamidestructure-activity relationshipdesign and synthesis
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