SYNTHESIS AND TESTING OF MALE CONTRACEPTIVE AGENTS

这项提议的长期目标是开发一种安全的非 具有睾丸后作用模式的荷尔蒙口服男性避孕药。 这项建议是基于观察到的安全口服酮康唑 人类杀真菌剂导致精子射精，这是 固定的。给大鼠灌注酮康唑可使它们 不孕不育。基于酮康唑(1)的结构，它是一种N- 通过取代1(H)-咪唑，合成了一系列 类似的C-取代咪唑(2)用于评价。

The long-term objective of this proposal is to develop a safe non- hormonal oral male contraceptive that has post-testicular mode of action. The proposal is based on the observation that ketoconazole, a safe oral human fungicide causes, causes ejaculation of spermatozoa which are immobilized. Administration of ketoconazole to rats renders them infertile. Based on the structure of ketoconazole (1), which is a N- substituted 1 (H)-imidazole, it is proposed to synthesize a series of analogous C-substituted imidazoles (2) for evaluation.