Useful β-turn mimetics having three-dimensional diversity
Useful β-turn mimetics having three-dimensional diversity
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
中文摘要
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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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
Investigation of the bioactive conformation of Histamine H3/H4 receptor antagonists by the conformational restriction strategy
通过构象限制策略研究组胺 H3/H4 受体拮抗剂的生物活性构象
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.
Investigation of the Bioactive Conformation of Histamine H_3 ReceptorAntagonists by the Cyclopropylic Strain-Based Conformational Restriction Strategy
基于环丙基菌株的构象限制策略研究组胺H_3受体拮抗剂的生物活性构象
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.
Structure determination of Pd-catalyst supported on S-terminated GaAs(001) using DFT calculation
使用 DFT 计算确定 S 端接 GaAs(001) 负载的 Pd 催化剂的结构
DOI:
--
发表时间:
2010
期刊:
Physica Status Solidi C : Current Topics in Solid State Physics 7
影响因子:
--
作者:
[Akira Ishii, Hiroki Asano, Mami Yokoyama, Shiro Tsukamoto, Satoshi Shuto, Mitsuhiro Arisawa]
通讯作者:
Mitsuhiro Arisawa
共 29 条
A Versatile Strategy for Developing Long-Acting Ligands by Ligand-Phospholipid Conjugation
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批准号:16K15136
-
项目类别:Grant-in-Aid for Challenging Exploratory Research
-
资助金额:$2.33万
-
财政年份:2016
-
负责人:SHUTO Satoshi
-
依托单位:
Medicinal chemical study by the three-dimensional structural diversity-oriented strategy based on the characteristic steric and stereoelectronic features of cyclopropane
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批准号:24390023
-
项目类别:Grant-in-Aid for Scientific Research (B)
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资助金额:$10.23万
-
财政年份:2012
-
负责人:SHUTO Satoshi
-
依托单位:
Investigation of the mechanism of insulin secretion via Ca
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批准号:23659049
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项目类别:Grant-in-Aid for Challenging Exploratory Research
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资助金额:$2.41万
-
财政年份:2011
-
负责人:SHUTO Satoshi
-
依托单位:
Development of ligands active specifically in intracellular Ca^<2+>-mobilizing second messenger system
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批准号:17390027
-
项目类别:Grant-in-Aid for Scientific Research (B)
-
资助金额:$7.01万
-
财政年份:2005
-
负责人:SHUTO Satoshi
-
依托单位:
Development of histamine H_3 receptor selective ligands based on the versatile chiral cyclopropane units.
-
批准号:15590096
-
项目类别:Grant-in-Aid for Scientific Research (C)
-
资助金额:$2.24万
-
财政年份:2003
-
负责人:SHUTO Satoshi
-
依托单位:
Development of New Silicon Tethers and Their Application to the Synthesis of Anti-HIV Nucleosides
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批准号:13672203
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项目类别:Grant-in-Aid for Scientific Research (C)
-
资助金额:$2.56万
-
财政年份:2001
-
负责人:SHUTO Satoshi
-
依托单位:
A Noven Radical Ring-Enlargement Reaction : The Reaction Mechanism and the Medicinal Chemical Application
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批准号:11672095
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项目类别:Grant-in-Aid for Scientific Research (C)
-
资助金额:$2.18万
-
财政年份:1999
-
负责人:SHUTO Satoshi
-
依托单位:
海外基金