SYNTHESIS AND TESTING OF MALE CONTRACEPTIVE AGENTS

这项建议的长远目标是发展一个安全的非- 激素口服男性避孕药，具有睾丸后作用模式。 该建议是基于观察到酮康唑，一种安全的口服 人类杀真菌剂导致，导致精子射精， 无法动弹 对大鼠施用酮康唑使其 不能生育 基于酮康唑（1）的结构，其为N- 取代的1（H）-咪唑，建议合成一系列 类似的C-取代的咪唑（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.