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Synthesis and biological evaluation of new series of benzamide derivatives containing urea moiety as sEH inhibitors. 2022
Ye Tian, and
Shuo Li, and
Peiyao Yang, and
Xiaolu Su, and
Jialu Liu, and
Xuening Lv, and
Kuan Dong, and
Ting Yang, and
Meibo Duan, and
Guangda Hu, and
Hao Yue, and
Yanping Sun, and
Yongjun Sun, and
Huimin Zhang, and
Zhidian Du, and
Zhenyu Miao, and
Minghui Tong, and
Yunlei Hou, and
Zibin Gao, and
Yanfang Zhao
Key Laboratory of Structure-Based Drug Design and Discovery, Ministry of Education, Shenyang Pharmaceutical University, Shenyang 110016, PR China.
The pharmacological inhibition of soluble epoxide hydrolase (sEH) was shown to reduce inflammation and pain. Herein, we described a series of newly synthesized sEH inhibitors with the trident-shaped skeleton. Intensive structural modifications led to the identification of compound B15 as a potent sEH inhibitor with an IC50 value of 0.03 ± 0.01 nM. Furthermore, compound B15 showed satisfactory metabolic stability in human liver microsomes with a half-time of 197 min. In carrageenan-induced inflammatory pain rat model, compound B15 exhibited a better therapeutic effect compared to t-AUCB and Celecoxib, which demonstrated the proof of potential as anti-inflammatory agents for pain relief.
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