Synthesis and inhibition of human acrosin and trypsin and acute toxicity of aryl 4-guanidinobenzoates

…, SR Mack, RA Anderson Jr, DP Waller…

文献索引：Kaminski, J. M.; Bauer, L.; Mack, S. R.; Anderson, R. A.; Waller, D. P.; Zaneveld, L. J. D. Journal of Medicinal Chemistry, 1986 , vol. 29, # 4 p. 514 - 519

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被引用次数: 24

摘要

The aryl 4-guanidinobenzoate, 4'-nitrophenyl4-guanidinobenzoate (NPGB), is a potent inhibitor of sperm acrosin, an enzyme with an essential function in the fertilization process. NPGB prevents fertilization in a number of animal species and is a good lead compound for the development of contraceptive agents. In order to assess the efficacy of other aryl 4- guanidinobenzoates as acrosin inhibitors, 24 of these compounds were synthesized. ...