NEW GOSSYPOL ANALOGUES FOR USE AS CONTRACEPTIVE

这项建议的目的是合成一些新的棉酚 用作男性避孕药的衍生品。事实上棉酚， 本身在中国身上已经被用作男性避孕药， 中国对廉价、可逆、无毒的男性避孕药的需求 发展中国家表示，新的更有效的棉酚衍生物 将在商业上取得成功。 将测试棉酚衍生物的抑制能力：1) 雄激素和雌激素与蛋白质结合；2)精子活力；3)精子 新陈代谢。此外，我们将准备足够数量的这些类似物 用于稍后的大鼠和仓鼠的活体研究(第二阶段)。另外，稍后 研究(第二阶段)可能包括测试这些棉酚衍生物 抑制克氏锥虫生长，杀灭疱疹病毒的能力。

The objective of this proposal is to synthesize some new gossypol derivatives for use as male contraceptives. The fact that gossypol, itself, is already being used as a male contraceptive agent in China, and the need for an inexpensive, reversible, non-toxic male contraceptive in developing countries indicates that new more potent gossypol derivatives will be commercially successful. The gossypol derivatives will be tested for ability to inhibit: 1) androgen and estrogen binding to proteins; 2) sperm motility; and 3) sperm metabolism. Also, we will prepare sufficient quantities of these analogues for later in vivo studies (phase II) with rats and hamsters. Also, later studies (phase II) may include testing these gossypol derivatives for ability to inhibit the growth of trypanosoma cruzi and killing herpes virus.