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Synthesis of a compound libraries inspired by privileged structures of natural products

受天然产物特殊结构启发的化合物库的合成

基本信息

批准号：
16310150
负责人：
ARIMOTO Hirokazu
金额：
$ 10.55万
依托单位：
Tohoku University (2005-2007)Nagoya University (2004)
依托单位国家：
日本
项目类别：
Grant-in-Aid for Scientific Research (B)
财政年份：
2004
资助国家：
日本
起止时间：
2004 至 2007
项目状态：
已结题

项目摘要

Natural product is a rich source of bioactive substances. In this research project, I focused on the preparation of a compound library based on important partial structures (the privileged structures) involved in natural products.At first I established the simple and efficient synthetic route to a plant growth regulator, theobroxide and its derivatives. Synthesis of a cytosolic phospholipase A2 inhibitor, pinnaic acid. Has also been established. Studies toward an antibiotic kendomycin, a cytotoxic material nakiterpiosin, aκ-opicid acceptor agonist, erinacine E were investigated, and their progress have been published as preliminary reports.In the course of the research for identification of novel endogenous bioactive low molecular-weight compounds, Prof. Akaike group at Kumamoto University and I have reported an existence of 8-nitro-cGMP in various cell lines. Preliminary studies suggested that the molecule should play an important roles at the time of infection and inflammation in our bodies. The design and synthesis of chemical probe molecule are underway.Furthermore, molecular shape of huge marine natural product, palytoxin, was elucidated by the synchrotron X-rays small angle scattering technique (SAXS). Direct observation of molecular shapes in solutions was accomplished with natural products for the first time. Palytoxin was proved to forms an associate dimer. Palytoxin have been shown to act on Na/K ATPase, and relationship of the associative nature with its biological activities should be an interesting future problem. Synthetic of a palytoxin-based library has investigated in this context.

天然产物是生物活性物质的丰富来源。在本研究项目中，我致力于天然产物重要部分结构（特权结构）化合物库的制备，首先建立了植物生长调节剂可可碱及其衍生物的简单有效的合成路线。胞浆型磷脂酶A2抑制剂羽叶酸的合成。也已经建立。对抗生素肯多霉素、细胞毒性物质裸片菌素、κ-阿片受体激动剂erinacine E进行了研究，并已发表初步报告。在鉴定新型内源性生物活性低分子量化合物的研究过程中，我和熊本大学赤池教授小组报告了各种细胞系中存在8-硝基-环鸟苷。初步研究表明，这种分子应该在我们体内的感染和炎症中发挥重要作用。利用同步辐射X射线小角散射技术（SAXS）对海洋天然产物海葵毒素的分子形态进行了研究。首次用天然产物直接观察溶液中的分子形状。海葵毒素可形成缔合二聚体。海葵毒素对Na/K ATP酶有一定的作用，其与Na/K ATP酶的结合性与其生物活性的关系是一个值得研究的问题。在此背景下，研究了基于palytoxin的文库的合成。

项目成果

期刊论文数量（25）

专著数量（0）

科研奖励数量（0）

会议论文数量（0）

专利数量（0）

Concise Synthesis of A Plant Growth Regulator Theobroxide

植物生长调节剂可可醇的简明合成

DOI：
发表时间：
2005
期刊：
J.Agr.Food Chem (in press)
影响因子：
0
作者：
Sugiura Hiroki;Yamaji Shunsuke;Yamada Takayoshi;Shimada Shigeru;Noguchi Takanori;Yokoya Tomohisa;H.Arimoto et al.
通讯作者：
H.Arimoto et al.

Molecular shape of palytoxin in aqueous solution