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: Hokkaido University
• 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
• 起止时间: 2009 至 2011
• 项目状态: 已结题
• 来源: https://kaken.nii.ac.jp/grant/KAKENHI-PROJECT-21390028/
• 关键词: βターン; ペプチドミメティック; シクロプロパン; MC4; Grb2; メラノコルチン受容体; ペプチドミメティックス; 活性配座; 配座制御; 三次元的多様性; 分子設計

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.

设计了具有立体化学多样性的β-转角模拟物，并发展了高效、立体选择性的合成方法。将模拟物应用于黑皮质素受体配体的开发，我们发现了一种高效的非肽先导物。因此，立体化学多样性导向的b-转角模拟物被证明可用于开发非肽先导物，特别是在配体的结合构象和受体的结构数据缺乏或记录不良的情况下。

项目成果

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

• 发表时间: 2012
• 期刊: Org.Biomol.Chem
• 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

• 发表时间: 2011
• 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
• 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

• 发表时间: 2010
• 期刊: Physica Status Solidi C : Current Topics in Solid State Physics 7
• 作者: Akira Ishii;Hiroki Asano;Mami Yokoyama;Shiro Tsukamoto;Satoshi Shuto;Mitsuhiro Arisawa
• 通讯作者: Mitsuhiro Arisawa