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Useful β-turn mimetics having three-dimensional diversity

Useful β-turn mimetics having three-dimensional diversity
具有三维多样性的有用的β-转角模拟物
批准号:
21390028
负责人:
SHUTO Satoshi
金额:
$11.56万
依托单位:
依托单位国家:
日本
项目类别:
Grant-in-Aid for Scientific Research (B)
财政年份:
2009
资助国家:
日本
项目状态:
已结题
起止时间:
2009 至 2011

项目摘要

项目成果

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相关文献

中文摘要
翻译
设计了面向立体化学多样性的b-转角模拟物,发展了高效、立体选择性的合成方法。将该模拟物应用于黑素皮质素受体配体的开发,我们发现了一种高效的非肽类先导化合物。因此,面向立体化学多样性的b-转弯模拟物被证明在开发非肽先导方面是有用的,特别是在缺乏配体的结合构象和受体的结构数据或缺乏文献记载的情况下。
英文摘要
The stereochemical diversity-oriented b-turn mimetics were designed and efficient and stereoselective synthetic method of them have been developed. Applying the mimetics to the development of melanocortin receptor ligands, we discovered a highly potent non-peptidic lead. Thus, the stereochemical diversity-oriented b-turn mimetics were shown to be useful in developing a non-peptidic lead, especially in cases where the binding conformation of the ligand and the structural data of the receptors are lacking or are poorly documented.
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会议论文
Cyclopropane-Based Stereochemical Diversity-Oriented Conformational Restriction Strategy : Histamine Analogs with the 4-Amino-2,3-methano-1-(1H-imidazol-4-y1) butane Structure as Highly Potent Histamine H3 and/or H4 Receptor Ligands
基于环丙烷的立体化学多样性导向的构象限制策略:具有 4-Amino-2,3-methano-1-(1H-imidazol-4-y1) 丁烷结构的组胺类似物作为高效组胺 H3 和/或 H4 受体配体
DOI: --
发表时间: 2012
期刊: Org.Biomol.Chem
影响因子: --
作者: [M.Watanabe, T.Kobayashi, T.Hirokawa, A.Yoshida, Y.Ito, S.Yamada, N.Orimoto, Y.Yamasaki, M.Arisawa, S.Shuto]
通讯作者: S.Shuto
DOI: --
发表时间: 2011
期刊:
影响因子: --
作者: [Kobayashi, T. , Watanabe, M., Hirokawa, T., Yamada, S., Arisawa, M., Shuto, S.]
通讯作者: S.
DOI: 10.1021/jm901848b
发表时间: 2010
期刊: J. Med. Chem
影响因子: --
作者: [M. Watanabe, T. Hirokawa, T. Kobayashi, A. Yoshida, Y. Ito, S. Yamada, N. Orimoto, Y. Yamasaki, M. Arisawa, S. Shuto]
通讯作者: S. Shuto
Alkene isomerization/enamide-ene and diene metathesis for the construction of indoles, quinolines, benzofurans and chromenes with a chiral cyclopropane substituent
烯烃异构化/烯酰胺-烯和二烯复分解用于构建具有手性环丙烷取代基的吲哚、喹啉、苯并呋喃和色烯
DOI: 10.1039/c0ob00597e
发表时间: 2011
期刊: Organic & Biomolecular Chemistry
影响因子: 3.2
作者: [Kobayashi, T., Arisawa, M., Shuto, S.]
通讯作者: S.
29
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