Creation of New Lead Compounds using Natural Resources and Metal Nanoparticle Catalysts

使用自然资源和金属纳米粒子催化剂创造新的铅化合物

• 批准号: 22K15252
• 负责人: SIRIMANGKALAKITTI NATCHANUN
• 金额: $ 3万
• 依托单位: Osaka University
• 依托单位国家: 日本
• 项目类别: Grant-in-Aid for Early-Career Scientists
• 财政年份: 2022
• 资助国家: 日本
• 起止时间: 2022-04-01 至 2024-03-31
• 项目状态: 已结题
• 来源: https://kaken.nii.ac.jp/en/grant/KAKENHI-PROJECT-22K15252/
• 关键词: natural product extract; metal catalyst; chemical diversification; lead compound

We accomplished to discover unprecedented chemical conversion and produce a new compound through a one-step reaction of substances present in the extract of marine sponge Petrosia (Strongylophora) sp.Chemical diversification of the substances present in the natural product extract with heat-treated EtOH produced a new, unexpected tetracyclic bromopyrrole-imidazole derivative, rac-6-OEt-cylindradine A. We also confirmed that it originated from naturally occurring (-)-cylindradine A via a new reaction pattern. Moreover, (-)-dibromophakellin and 4,5-dibromopyrrole-2-carboxylic acid as well as (-)-cylindradine A were reported herein for the first time in this genus. Studies on the possible reaction mechanism and bioactivities were also conducted. The results indicate that the direct chemical diversification of substances present in natural product extracts can be a speedy and useful strategy for the discovery of new compounds.

我们成功地发现了前所未有的化学转化，并通过海绵Petrosia (Strongylophora) sp.提取物中存在的物质的一步反应产生了一种新的化合物。天然产物提取物中存在的物质与热处理的乙氧乙酸的化学多样化产生了一种新的，意想不到的四环溴吡咯-咪唑衍生物。rac-6- oet - adine A.通过新的反应模式证实其来源于天然存在的(-)- adine A。此外，(-)-二溴吡咯啉和4,5-二溴吡咯-2-羧酸以及(-)-圆柱胺A在该属中首次报道。并对其可能的反应机理和生物活性进行了研究。结果表明，天然产物提取物中存在的物质的直接化学多样化可以成为发现新化合物的一种快速而有用的策略。

项目成果

A New Tetracyclic Bromopyrrole-Imidazole Derivative through Direct Chemical Diversification of Substances Present in Natural Product Extract from Marine Sponge Petrosia (Strongylophora) sp.

• DOI: 10.3390/molecules28010143
• 发表时间: 2022-12-24
• 期刊: MOLECULES
• 影响因子: 4.6
• 作者: Sirimangkalakitti, Natchanun;Harada, Kazuo;Yamada, Makito;Arai, Masayoshi;Arisawa, Mitsuhiro
• 通讯作者: Arisawa, Mitsuhiro