期刊论文

Zhu, Xiao-Lei;Yang, GF

英文

JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY

0021-8561

2023

71

47

18292-18300

10.1021/acs.jafc.3c02158

The research was supported in part by the National Key Research and Development Program of China (2022YFD1700204), the Key Research and Development Program of Hubei Province (2020BBA052), and the National Natural Science Foundation of China (no. 21977035, 21837001, and 21772057).

本校为第一且通讯机构

Scaffold hopping strategy has become one of the most successful methods in the process of molecular design. Seeking to develop novel succinate dehydrogenase inhibitors (SDHIs), we employed a scaffold hopping strategy to design compounds featuring geminate dichloralkenes (gem-dichloralkenes) fragment. After stepwise modifications, a series of N-cyclopropyl-dichloralkenes-pyrazole-carboxamide derivatives was synthesized. Among them, compounds G28 (IC50 = 26.00 nM) and G40 (IC50 = 27.00 nM) were identified as the best inhibitory activity against p...