title: 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.
authors.affiliation: Department of Medicinal Chemistry, School of Pharmacy, Second Military Medical University, Shanghai 200433, PR China.
authors.forename: Wei
authors.initials: W
authors.lastname: Tian
authors.forename: Guangqian
authors.initials: G
authors.lastname: Han
authors.forename: Ju
authors.initials: J
authors.lastname: Zhu
authors.forename: Jingjing
authors.initials: J
authors.lastname: Qi
authors.forename: Qianqian
authors.initials: Q
authors.lastname: Chen
authors.forename: Juntao
authors.initials: J
authors.lastname: Zhao
authors.forename: Canhui
authors.initials: C
authors.lastname: Zheng
authors.forename: Ling
authors.initials: L
authors.lastname: Zhang
authors.forename: Youjun
authors.initials: Y
authors.lastname: Zhou
authors.forename: Jiaguo
authors.initials: J
authors.lastname: Lv
mesh_terms: D000176:Acrosin / Q000037:antagonists & inhibitors / Q000378:metabolism; D000577:Amides / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics; D001665:Binding Sites; D020134:Catalytic Domain; D018360:Crystallography, X-Ray; D006207:Half-Life; D006801:Humans; D008968:Molecular Conformation; D062105:Molecular Docking Simulation; D011480:Protease Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000493:pharmacokinetics; D011720:Pyrazoles / Q000138:chemical synthesis* / Q000737:chemistry* / Q000493:pharmacokinetics
chemical_list: C585743:AQ-E5 compound; D000577:Amides; D011480:Protease Inhibitors; D011720:Pyrazoles; C031280:pyrazole; D000176:Acrosin