BIOLOGICAL PROPERTIES OF GOSSYPOL AND DERIVATIVES

棉酚及其衍生物的生物特性

• 批准号: 3856435
• 负责人: DAVID L VANDER JAGT
• 金额: --
• 依托单位: UNIVERSITY OF NEW MEXICO
• 依托单位国家: 美国
• 资助国家: 美国
• 起止时间: 至
• 项目状态: 未结题
• 来源: https://reporter.nih.gov/project-details/3856435
• 关键词: Plasmodium falciparum; aldehyde reductase; antimalarial agents; antiprotozoal agents; antiviral agents; bioenergetics; chemical structure function; drug adverse effect; drug design /synthesis /production; enzyme inhibitors; gestational diabetes mellitus; herpes simplex virus 2; lactate dehydrogenases; liver metabolism; parasitic disease chemotherapy; spermatogenesis inhibitor; transferase; trypanosomiasis

Derivatives of the disesquiterpene gossypol will be synthesized. This primarily involves modification of the aldehyde functional groups of gossypol. Gossypol and derivatives will be evaluated in three different biological assay systems. 1. Gossypol and derivatives will be evaluated for their antiparasitic activity against the malarial parasite P.falciparum. Activity will be compared with the ability of the drugs to inhibit parasite lactate dehydrogenase, the putative target. 2. Gossypol and derivatives will be evaluated for their antiviral properties against herpes simplex type II. 3. Gossypol and derivatives will be evaluated for their properties as inhibitors of aldose reductase from human placenta. This enzyme is the target for drugs which may be useful in the treatment of diabetic complications.

合成了棉酚的二倍半萜衍生物。 这主要涉及醛官能团的修饰。 棉酚组。 棉酚及其衍生物将在 三种不同的生物测定系统。 1.棉酚及其衍生物将被评估其 抗疟原虫恶性疟原虫的抗寄生虫活性。 活性将与药物抑制 寄生虫乳酸脱氢酶，推定的目标。 2.棉酚及其衍生物的抗病毒作用将被评估 对单纯疱疹病毒II型。 3.棉酚及其衍生物的性能将进行评估 作为来自人胎盘的醛糖还原酶的抑制剂。 这种酶 是药物的靶点， 糖尿病并发症