避孕药胍苯酸酯(EGB)精子顶体蛋白酶抑制剂的合成

THE SYNTHESIS OF HUMAN SPERM ACROSIN INHIBITOR OF ARYL 4-GUANIDINOBENZOATE

本文报道了一种新型避孕药——精子顶体蛋白酶抑制剂4-胍基苯甲酸-(4′-苯甲酸苯乙酯(EGB)(4-Carboethoxyphenyl-4′-Guanidinobenzoate·HCl)的合成方法。

The 4-Carboethoxyphenyl 4'-Guanidinobenzoate· HCI is a potent inhibitor of sperm acrosin, an enzyme with an essential function in the fertilization process. The aryl 4-guanidinobenzoate synthesized from FDA-approved phenols was less toxic than nonoxynol-9,and it is of interest for further development and testing as a nonhormonal contraceptive agent.