Synthesis and biological evaluation of homopiperazine derivatives with beta-aminoacyl group as dipeptidyl peptidase IV inhibitors.

Ahn JH; Park WS; Jun MA; Shin MS; Kang SK; Kim KY; Rhee SD; Bae MA; Kim KR; Kim SG; Kim SY; Sohn SK; Kang NS; Lee JO; Lee DH; Cheon HG; Kim SS

首页> 外文期刊>Bioorganic and Medicinal Chemistry Letters >Synthesis and biological evaluation of homopiperazine derivatives with beta-aminoacyl group as dipeptidyl peptidase IV inhibitors.

【24h】

Synthesis and biological evaluation of homopiperazine derivatives with beta-aminoacyl group as dipeptidyl peptidase IV inhibitors.

机译：具有β-氨基酰基作为二肽基肽酶IV抑制剂的高哌嗪衍生物的合成和生物学评估。

获取原文

获取原文并翻译 | 示例

掌桥外文数据库（机构版） >>

开具论文收录证明 >>

文献代查 >>

页面导航

摘要
著录项
相似文献
相关主题

摘要

Compounds with homopiperazine skeleton are designed to find a potent DPP-IV inhibitor without inhibiting CYP. Thus a series of beta-aminoacyl-containing homopiperazine derivatives was synthesized and evaluated. Compounds with acid moiety were found to be potent inhibitors of DPP-IV without inhibiting CYP 3A4. More specifically, compound 7m showed nanomolar activity with no inhibition towards five subtypes of CYPs, was considered as a prototype for further derivatization. Based on its X-ray co-crystal structure with human DPP-IV, we identified compounds 7s and 7t which showed good in vitro activity, no CYP inhibition, and good selectivity.

机译：设计具有高哌嗪骨架的化合物以找到有效的DPP-IV抑制剂而不抑制CYP。因此，合成并评估了一系列含β-氨基酰基的高哌嗪衍生物。发现具有酸部分的化合物是DPP-IV的有效抑制剂，而没有抑制CYP 3A4。更具体地说，化合物7m显示出纳摩尔活性，对CYP的5个亚型没有抑制作用，被认为是进一步衍生化的原型。基于其与人DPP-IV的X射线共晶体结构，我们鉴定出化合物7s和7t具有良好的体外活性，无CYP抑制作用和良好的选择性。

著录项

来源
《Bioorganic and Medicinal Chemistry Letters》 |2008年第24期|共5页
作者
Ahn JH; Park WS; Jun MA; Shin MS; Kang SK; Kim KY; Rhee SD; Bae MA; Kim KR; Kim SG; Kim SY; Sohn SK; Kang NS; Lee JO; Lee DH; Cheon HG; Kim SS;
展开▼
作者单位

展开▼
收录信息
原文格式 PDF
正文语种 eng
中图分类药学;生物化学;
关键词
Roman Numeral IV; CYP; inhibitors; derivatives; g lt; 3gt;

机译：罗马数字IV;CYP;抑制剂;衍生物;g 3;

相似文献

外文文献
中文文献
专利

1. Synthesis and biological evaluation of homopiperazine derivatives with beta-aminoacyl group as dipeptidyl peptidase IV inhibitors. [J] . Ahn JH, Park WS, Jun MA, Bioorganic and Medicinal Chemistry Letters . 2008,第24期

机译：具有β-氨基酰基作为二肽基肽酶IV抑制剂的高哌嗪衍生物的合成和生物学评估。
2. Discovery of beta-aminoacyl containing thiazolidine derivatives as potent and selective dipeptidyl peptidase IV inhibitors. [J] . Park WS, Kang SK, Jun MA, Bioorganic and Medicinal Chemistry Letters . 2011,第5期

机译：发现含有β-氨基酰基的噻唑烷衍生物作为有效的和选择性的二肽基肽酶IV抑制剂。
3. Synthesis and evaluation of pyrazolidine derivatives as dipeptidyl peptidase IV (DP-IV) inhibitors. [J] . Ahn JH, Kim JA, Kim HM, Bioorganic and Medicinal Chemistry Letters . 2005,第5期

机译：吡唑烷衍生物作为二肽基肽酶IV（DP-IV）抑制剂的合成和评估。
4. Classification analysis using support vector machine, decision tree, and neural network with principal component analysis to determine molecular structure relationship from its biological activity on dipeptidyl peptidase IV inhibitors [C] . Haris Hamzah, Alhadi Bustamam, Arry Yanuar, International Conference on Science and Applied Science . 2020

机译：使用支撑向量机，决策树和神经网络具有主成分分析的分类分析，从而确定二肽基肽酶IV抑制剂的生物活性分子结构关系
5. Total synthesis and biological evaluation of fluoroolefin-containing dipeptide isosteres as inhibitors of dipeptidyl peptidase IV (CD26). [D] . Lin, Jian. 1998

机译：作为二肽基肽酶IV（CD26）抑制剂的含氟烯烃的二肽等位基因的全合成和生物学评估。
6. Design of new disubstituted imidazo12-bpyridazine derivatives as selective Haspin inhibitors. Synthesis binding mode and anticancer biological evaluation [O] . Jonathan Elie, Omid Feizbakhsh, Nathalie Desban, 2020

机译：新的二取代的咪唑（吡啶嗪衍生物为选择性HAPIN抑制剂的设计。合成结合模式和抗癌生物学评估
7. Synthesis, Evaluation and Molecular Docking of Thiazolopyrimidine Derivatives as Dipeptidyl Peptidase IV Inhibitors [O] . Mani Sharma, Monica Gupta, Divya Singh, 2012

机译：噻唑吡啶胺衍生物作为二肽基肽酶IV抑制剂的合成，评价和分子对接

Synthesis and biological evaluation of homopiperazine derivatives with beta-aminoacyl group as dipeptidyl peptidase IV inhibitors.

摘要

著录项

相似文献

相关主题

期刊订阅