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Synthesis and biological evaluation of new series of benzamide derivatives containing urea moiety as sEH inhibitors.
Tian, Ye; Li, Shuo; Yang, Peiyao; Su, Xiaolu; Liu, Jialu; Lv, Xuening; Dong, Kuan; Yang, Ting; Duan, Meibo; Hu, Guangda; Yue, Hao; Sun, Yanping; Sun, Yongjun; Zhang, Huimin; Du, Zhidian; Miao, Zhenyu; Tong, Minghui; Hou, Yunlei; Gao, Zibin; Zhao, Yanfang.
Afiliação
  • Tian Y; Key Laboratory of Structure-Based Drug Design and Discovery, Ministry of Education, Shenyang Pharmaceutical University, Shenyang 110016, PR China.
  • Li S; State Key Laboratory Breeding Base-Hebei Province Key Laboratory of Molecular Chemistry for Drug, Hebei University of Science and Technology, Shijiazhuang, PR China.
  • Yang P; Key Laboratory of Structure-Based Drug Design and Discovery, Ministry of Education, Shenyang Pharmaceutical University, Shenyang 110016, PR China.
  • Su X; State Key Laboratory Breeding Base-Hebei Province Key Laboratory of Molecular Chemistry for Drug, Hebei University of Science and Technology, Shijiazhuang, PR China.
  • Liu J; Key Laboratory of Structure-Based Drug Design and Discovery, Ministry of Education, Shenyang Pharmaceutical University, Shenyang 110016, PR China.
  • Lv X; State Key Laboratory Breeding Base-Hebei Province Key Laboratory of Molecular Chemistry for Drug, Hebei University of Science and Technology, Shijiazhuang, PR China.
  • Dong K; Key Laboratory of Structure-Based Drug Design and Discovery, Ministry of Education, Shenyang Pharmaceutical University, Shenyang 110016, PR China.
  • Yang T; State Key Laboratory Breeding Base-Hebei Province Key Laboratory of Molecular Chemistry for Drug, Hebei University of Science and Technology, Shijiazhuang, PR China.
  • Duan M; Key Laboratory of Structure-Based Drug Design and Discovery, Ministry of Education, Shenyang Pharmaceutical University, Shenyang 110016, PR China.
  • Hu G; State Key Laboratory Breeding Base-Hebei Province Key Laboratory of Molecular Chemistry for Drug, Hebei University of Science and Technology, Shijiazhuang, PR China.
  • Yue H; Key Laboratory of Structure-Based Drug Design and Discovery, Ministry of Education, Shenyang Pharmaceutical University, Shenyang 110016, PR China.
  • Sun Y; State Key Laboratory Breeding Base-Hebei Province Key Laboratory of Molecular Chemistry for Drug, Hebei University of Science and Technology, Shijiazhuang, PR China.
  • Sun Y; State Key Laboratory Breeding Base-Hebei Province Key Laboratory of Molecular Chemistry for Drug, Hebei University of Science and Technology, Shijiazhuang, PR China.
  • Zhang H; State Key Laboratory Breeding Base-Hebei Province Key Laboratory of Molecular Chemistry for Drug, Hebei University of Science and Technology, Shijiazhuang, PR China.
  • Du Z; State Key Laboratory Breeding Base-Hebei Province Key Laboratory of Molecular Chemistry for Drug, Hebei University of Science and Technology, Shijiazhuang, PR China.
  • Miao Z; 3D BioOptima Co,. Ltd., Suzhou 215104, PR China.
  • Tong M; 3D BioOptima Co,. Ltd., Suzhou 215104, PR China.
  • Hou Y; Key Laboratory of Structure-Based Drug Design and Discovery, Ministry of Education, Shenyang Pharmaceutical University, Shenyang 110016, PR China.
  • Gao Z; State Key Laboratory Breeding Base-Hebei Province Key Laboratory of Molecular Chemistry for Drug, Hebei University of Science and Technology, Shijiazhuang, PR China. Electronic address: zbgao74@163.com.
  • Zhao Y; Key Laboratory of Structure-Based Drug Design and Discovery, Ministry of Education, Shenyang Pharmaceutical University, Shenyang 110016, PR China. Electronic address: yanfangzhao@126.com.
Bioorg Med Chem Lett ; 70: 128805, 2022 08 15.
Article em En | MEDLINE | ID: mdl-35598794
ABSTRACT
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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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Inibidores Enzimáticos / Epóxido Hidrolases Idioma: En Ano de publicação: 2022 Tipo de documento: Article
Texto completo
Imprimir
XML
PubMed Links
Buscar no Google

Texto completo: 1 Base de dados: MEDLINE Assunto principal: Inibidores Enzimáticos / Epóxido Hidrolases Idioma: En Ano de publicação: 2022 Tipo de documento: Article