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Peptide synthesis Catalyzed by Micellur Models of Metalloenzymes

金属酶胶束模型催化的肽合成

基本信息

批准号：
60470097
负责人：
TAGAKI Waichiro
金额：
$ 2.69万
依托单位：
Osaka City University
依托单位国家：
日本
项目类别：
Grant-in-Aid for General Scientific Research (B)
财政年份：
1985
资助国家：
日本
起止时间：
1985 至 1987
项目状态：
已结题

项目摘要

The purpose of this project was to develope an efficient method for the synthesis of peptides by the use of some micellar systems containing lipophilic ligandmetal ion complexes as the catalysts. Various lipophilic ligands were newly synthesized; they contain imidazole group(s) for the chelation with metal ions and nucleophilic hydroxyl group(s) attack ester substrates. These ligands were allowed to form complexes with metal ions, Zn^<2+> and Cu^<2+>, in aqueous micelles of cationic, anionic, or non-ionic surfactants, as well as in reverse micelles of AOT surfactant inhexane. Some of these co-micellar systems exhibited remarkable catalytic activities in the hydrolysis of active esters, such as p-nitrophenyl picolinate. They were also active in the acyl transfer reactions between alcohols in AOT reverse micelles when DMF was used as the core solvent.Unfortunately, however, the above systems did show enough activity for the condensation of amino acid esters to form peptides with reasonable yields. Further works are required to design more powerful catalysts. With regard to this, we were able to prepare a novel surfactant ligand and found it to be a remarkably active catalyst when complexed with Cu^<2+> ion, although the applicability to peptide synthehas not yet been examined.

本课题的目的是发展一种以亲脂性配体-金属离子络合物为催化剂的胶束体系合成多肽的有效方法。新合成了各种亲脂性配体，它们含有咪唑基团，用于与金属离子螯合，亲核羟基攻击酯底物。在阳离子、阴离子或非离子表面活性剂的水胶束以及AOT表面活性剂在己烷中的反胶束中，这些配体可以与金属离子Zn ^2+和Cu^2+形成络合物。其中一些共胶束体系对吡啶甲酸对硝基苯酚酯等活性酯的水解反应表现出显著的催化活性。在以DMF为核心溶剂的AOT反胶束体系中，它们在醇类间的酰基转移反应中也表现出一定的活性，但在氨基酸酯的缩合反应中，它们表现出了足够的活性。需要进一步的工作来设计更强大的催化剂。考虑到这一点，我们能够制备一种新的表面活性剂配体，并发现它与Cu^2+离子络合时是一种非常活性的催化剂，尽管对肽合成的适用性还没有被检验。