ANTIVIRAL/BIOACTIVE COMPOUNDS--SYNTHESIS AND CHEMISTRY

抗病毒/生物活性化合物——合成和化学

• 批准号: 2838502
• 负责人: ELIAS J COREY
• 金额: $ 90.13万
• 依托单位: HARVARD UNIVERSITY
• 依托单位国家: 美国
• 财政年份: 1984
• 资助国家: 美国
• 起止时间: 1984-12-01 至 2000-11-30
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/2838502
• 关键词: antiAIDS agent; antiinflammatory agents; antiviral agents; brefeldin A; catalyst; chemical structure function; cyclic AMP; drug design /synthesis /production; drug screening /evaluation; eicosanoid metabolism; forskolin; immunosuppressive; lipoxygenase; prostaglandins; serotonin inhibitor; stereochemistry; stereoisomer; thromboxanes; transplantation

The overall objective of this research is the study of fundamental aspects of synthetic organic and bioorganic chemistry and the application of these disciplines to important problems of biochemistry and medicine. Specific projects for study include the following: (1) synthesis of therapeutic agents against human immunodeficiency virus; (2) synthesis of immunosuppressants for organ transplants; (3) synthesis of the antibiotic, crinipellin A; (4) synthesis of the hormonal substance, miroestrol; (5) synthesis of the activator of cyclic AMP synthase, forskolin; (6) synthesis of the antiinflammatory agent, pseudopterosin E; (7) synthesis of the inhibitor of protein translocation and processing, brefeldin A; (8) synthesis of the inhibitors of biosynthesis of initiation factor 4D; (9) synthesis of new serotonin uptake inhibitors. Bioorganic studies are proposed on the binding of prostaglandins and thromboxanes to their receptors, the 12-lipoxygenase pathway of eicosanoid action, and cholesterol biosynthesis. Finally, new methodology which is needed in organic synthesis will be investigated, especially methods for enantioselective and catalytic synthesis.

本研究的总体目标是研究基本方面 合成有机和生物有机化学及其应用 生物化学和医学的重要问题。 具体 研究项目包括：（1）合成治疗 抗人类免疫缺陷病毒的药物;（2）合成 用于器官移植的免疫抑制剂;（3）抗生素的合成， 海鞘素A;（4）激素物质miroestrol的合成;（5） 环腺苷酸合成酶激活剂毛喉素的合成;（6）合成 （7）合成抗肿瘤剂假蝶呤E; 蛋白质转运和加工抑制剂，布雷菲德菌素A;（8） 起始因子4D生物合成抑制剂的合成;（9） 合成新的5-羟色胺摄取抑制剂。 生物有机研究是 提出了对结合的arylandins和血栓烷，以其 受体，类花生酸作用的12-脂氧合酶途径，和 胆固醇生物合成 最后，需要新的方法， 将研究有机合成，特别是方法 对映选择性和催化合成。

项目成果

Generation of leukotriene C4 from a subclass of mast cells differentiated in vitro from mouse bone marrow.

从小鼠骨髓体外分化的肥大细胞亚类产生白三烯 C4。

• DOI: 10.1073/pnas.79.15.4665
• 发表时间: 1982
• 期刊: Proceedings of the National Academy of Sciences of the United States of America
• 影响因子: 11.1
• 作者: Razin,E;Mencia-Huerta,JM;Lewis,RA;Corey,EJ;Austen,KF
• 通讯作者: Austen,KF