Synthesis and acrosin inhibitory activities of 5-phenyl-1H-pyrazole-3-carboxylic acid amide derivatives.

Abstract

A series of novel 5-phenyl-1H-pyrazole-3-carboxylic acid amide derivatives were designed, synthesized, and their acrosin inhibitory activities in vitro were evaluated. The results of the acrosin inhibitory activity showed that all target compounds were more potent than control TLCK. Compounds AQ-A1, AQ-D3, AQ-D4, AQ-E4 and AQ-E5 exhibited stronger acrosin inhibitory activities than control ISO-1. Especially, compound AQ-E5 displayed the most potent acrosin inhibitory activity in all the compounds, with an IC50 of 0.01μmol/mL. This study provided a new structural class for the development of novel acrosin inhibitory agents.

DOI: 10.1016/j.bmcl.2013.05.031

Cite this paper

@article{Tian2013SynthesisAA, title={Synthesis and acrosin inhibitory activities of 5-phenyl-1H-pyrazole-3-carboxylic acid amide derivatives.}, author={Wei Tian and Guangqian Han and Ju Zhu and Jingjing Qi and Qianqian Chen and Juntao Zhao and Canhui Zheng and Ling Zhang and Youjun Zhou and Jiaguo Lv}, journal={Bioorganic & medicinal chemistry letters}, year={2013}, volume={23 14}, pages={4177-84} }