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.
Copyright © 2011 Elsevier Ltd. All rights reserved.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Acrosin / antagonists & inhibitors*
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Carboxylic Acids / chemical synthesis*
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Carboxylic Acids / chemistry
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Carboxylic Acids / pharmacology
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Contraceptive Agents / chemical synthesis*
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Contraceptive Agents / chemistry
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Contraceptive Agents / pharmacology
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Drug Design
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Fertilization / physiology
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Humans
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Male
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Molecular Targeted Therapy
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Pyrazoles / chemical synthesis*
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Pyrazoles / chemistry
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Pyrazoles / pharmacology
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Serine Proteinase Inhibitors / chemical synthesis*
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Serine Proteinase Inhibitors / chemistry
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Serine Proteinase Inhibitors / pharmacology
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Software*
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Structure-Activity Relationship
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Tosyllysine Chloromethyl Ketone / chemistry
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Tosyllysine Chloromethyl Ketone / metabolism
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Tosyllysine Chloromethyl Ketone / pharmacology
Substances
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Carboxylic Acids
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Contraceptive Agents
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Pyrazoles
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Serine Proteinase Inhibitors
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Tosyllysine Chloromethyl Ketone
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Acrosin