Synthesis and Design of Structures of Biologically Active Compounds

生物活性化合物的合成与结构设计

• 批准号: 02303017
• 负责人: SHIOIRI Takayuki
• 金额: $ 7.17万
• 依托单位: Nagoya City University
• 依托单位国家: 日本
• 项目类别: Grant-in-Aid for Co-operative Research (A)
• 财政年份: 1990
• 资助国家: 日本
• 起止时间: 1990 至 1992
• 项目状态: 已结题
• 来源: https://kaken.nii.ac.jp/grant/KAKENHI-PROJECT-02303017/
• 关键词: Biologically active compounds; Efficient synthesis; Structures; Peptides; Sugars; Macrolides; Design of drugs; Physicochemical approach; 物理化学的アプロ-チ; 効率的合成法

The purpose of this research project is as follows : (1) exploitation of efficient synthetic methods for biologically active compounds, (2) identification of the molecular structures which are essential to exhibit biological activities of the compounds, (3) clarification of life of animals and plants on molecular levels, and (4) design of new biologically active compounds useful for human life. The research groups have consisted of 16 professors and the research projects have been divided into four : (1) investigations of biologically active peptides on their synthetic methods and on the structures responsible for their biological activities, (2) investigations of sugars and macrolides on their synthetic methods and on the structures responsible for their biological activities, (3) development of drugs useful for the treatment of diseases on circulatory organs and central nervous system in addition to development of anticancer drugs, and (4) investigations on structures responsible for biological activities by the physicochemical methods. We have successfully pursued all of these projects, and our projects ended to have a great promise of the future development on the syntheses and design of structures of biologically active compounds.

这项研究的目的是：(1)开发有效的生物活性化合物的合成方法；(2)鉴定展示化合物生物活性所必需的分子结构；(3)从分子水平上阐明动植物的生命；(4)设计对人类生活有用的新的生物活性化合物。研究小组由16名教授组成，研究项目分为四个：(1)生物活性多肽的合成方法和负责其生物活性的结构的研究；(2)糖和大环内酯类化合物的合成方法和负责其生物活性的结构的研究；(3)除抗癌药物的开发外，用于治疗循环系统和中枢神经系统疾病的药物的开发；(4)用物理化学方法研究具有生物活性的结构。我们已经成功地完成了所有这些项目，我们的项目最终在生物活性化合物的合成和结构设计方面有了很大的发展前景。

项目成果

K.Fukase: "4ーPivaloylaminobenzyl Ether,a New Temporary Profection for Hydroxyl Functions" Tetrahedron Letters. 32. 3557-3558 (1991)

K. Fukase：“4-新戊酰氨基苄基醚，羟基功能的新临时保护”四面体快报 32. 3557-3558 (1991)

T.Igarashi: "Structure of a mouse immunoglobulin G that lacks the entire C_H1 domain:Protein sequencing and smallーangle Xーray scattering studies" Biochemistry. 29. 5727-5733 (1990)

T.Igarashi：“缺乏整个 C_H1 结构域的小鼠免疫球蛋白 G 的结构：蛋白质测序和小角 X 射线散射研究”《生物化学》29. 5727-5733 (1990)。

N.Nakajima: "Facile Total Synthesis of Carbonolides by wittigーHorner MacroーCyclization and Stereospecific Epoxidation" Chem.Pharm.Bull.39. 64-74 (1991)

N.Nakajima：“通过 wittig-Horner 大环化和立体定向环氧化轻松全合成碳内酯”Chem.Pharm.Bull.39 (1991)。

Toshimasa Ishida: "Conformational feature of aureobasidin E,a new type of potent antifungal antibiotic" J.Chem.Soc.Chem.Commun.1231-1233 (1992)

Toshimasa Ishida：“aureobasidin E 的构象特征，一种新型强效抗真菌抗生素”J.Chem.Soc.Chem.Commun.1231-1233 (1992)

S.Takano: "A New Enantiospecific Route to(-)ーKanic Acid Via the Intramoleclar pausonーKhand Reaction" J.Chem.Soc.,Chem.Commun.169-170 (1992)

S.Takano：“通过分子内 pauson-Khand 反应生成 (-)-Kanic Acid 的新对映体特异性路线”J.Chem.Soc.,Chem.Commun.169-170 (1992)