title: Synthesis and acrosin inhibitory activities of substituted ethyl 5-(4-aminophenyl)-1H-pyrazole-3-carboxylate derivatives.
abstract: A series of novel ethyl 5-(4-aminophenyl)-1H-pyrazole-3-carboxylate derivatives were designed and synthesized and their in vitro acrosin inhibitory activities were evaluated. Most of the compounds exhibited acrosin inhibitory activities. Among them, three compounds (5l, 5n, and 5v) were more potent than that of the control TLCK. These provide a new structural type for the development of novel contraceptive acrosin inhibitory agents.
authors: Department of Medicinal Chemistry, School of Pharmacy, Second Military Medical University, Shanghai 200433, PR China.
authors: Jingjing
authors: J
authors: Qi
authors: Ju
authors: J
authors: Zhu
authors: Xuefei
authors: X
authors: Liu
authors: Lili
authors: L
authors: Ding
authors: Canhui
authors: C
authors: Zheng
authors: Guangqian
authors: G
authors: Han
authors: Jiaguo
authors: J
authors: Lv
authors: Youjun
authors: Y
authors: Zhou
mesh_terms: D000176:Acrosin / Q000037:antagonists & inhibitors*; D002264:Carboxylic Acids / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D003270:Contraceptive Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D015195:Drug Design; D005306:Fertilization / Q000502:physiology; D006801:Humans; D008297:Male; D058990:Molecular Targeted Therapy; D011720:Pyrazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D015842:Serine Proteinase Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D012984:Software; D013329:Structure-Activity Relationship; D014107:Tosyllysine Chloromethyl Ketone / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology
chemical_list: D002264:Carboxylic Acids; D003270:Contraceptive Agents; D011720:Pyrazoles; D015842:Serine Proteinase Inhibitors; D014107:Tosyllysine Chloromethyl Ketone; D000176:Acrosin