Synthesis of novel benzofuran isoxazolines as protein tyrosine phosphatase 1B inhibitors.

Ahmad G; Mishra PK; Gupta P; Yadav PP; Tiwari P; Tamrakar AK; Srivastava AK; Maurya R

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Synthesis of novel benzofuran isoxazolines as protein tyrosine phosphatase 1B inhibitors.

机译：新型苯并呋喃异恶唑啉作为蛋白质酪氨酸磷酸酶1B抑制剂的合成。

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PTPases are considered to be involved in the etiology of diabetes mellitus and neural diseases, such as Alzheimer's disease and Parkinson's disease. Therefore, PTPase inhibitors should be useful tools to study the role of PTPases in these diseases and other biological phenomena, and which can be developed into chemotherapeutic agents. In the present study, we have synthesized novel benzofuran isoxazolines 13-21 via 1,3-dipolar cycloaddition reaction using karanjin (1) and kanjone (2), isolated from Pongamia pinnata fruits. All the synthesized compounds were evaluated against PTPase enzyme. Compounds 19 and 20 displayed significant inhibitory activity with IC50 values 76 and 81 microM, respectively.

机译：PTP酶被认为与糖尿病和神经疾病例如阿尔茨海默氏病和帕金森氏病的病因有关。因此，PTPase抑制剂应该是研究PTPase在这些疾病和其他生物学现象中的作用的有用工具，并可以发展成为化学治疗剂。在本研究中，我们使用分离自Pongamia pinnata果实的karanjin（1）和kanjone（2）通过1,3-偶极环加成反应合成了新型苯并呋喃异恶唑啉13-21。所有合成的化合物均针对PTPase酶进行了评估。化合物19和20表现出明显的抑制活性，IC50分别为76和81 microM。

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《Bioorganic and Medicinal Chemistry Letters》 |2006年第8期|共5页
作者
Ahmad G; Mishra PK; Gupta P; Yadav PP; Tiwari P; Tamrakar AK; Srivastava AK; Maurya R;
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正文语种 eng
中图分类药学;生物化学;
关键词
Enzyme Inhibitors; Hypoglycemic Agents; Protein-Tyrosine-Phosphatase; 酶抑制剂; 降血糖药; 蛋白质酪氨酸磷酸酶;

机译：Enzyme Inhibitors;Hypoglycemic Agents;Protein-Tyrosine-Phosphatase;酶抑制剂;降血糖药;蛋白质酪氨酸磷酸酶;

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1. Synthesis of novel benzofuran isoxazolines as protein tyrosine phosphatase 1B inhibitors. [J] . Ahmad G, Mishra PK, Gupta P, Bioorganic and Medicinal Chemistry Letters . 2006,第8期

机译：新型苯并呋喃异恶唑啉作为蛋白质酪氨酸磷酸酶1B抑制剂的合成。
2. Synthesis of 3,5-disubstituted isoxazolines as protein tyrosine phosphatase 1B inhibitors [J] . Rakesh Maurya, Prasoon Gupta, Ghufran Ahmad, Medicinal chemistry research: an international journal for rapid communications on design and mechanisms of action of biologically active agents . 2008,第2a7期

机译：3,5-二取代异恶唑啉作为蛋白质酪氨酸磷酸酶1B抑制剂的合成
3. Design, synthesis, and evaluation of bromo-retrochalcone derivatives as protein tyrosine phosphatase 1B inhibitors. [J] . Liu Z, Lee W, Kim SN, Bioorganic and Medicinal Chemistry Letters . 2011,第12期

机译：设计，合成和评估作为蛋白酪氨酸磷酸酶1B抑制剂的溴-逆查尔酮衍生物。
4. Discovery and study of novel protein tyrosine phosphatase 1B inhibitors [C] . Qian Zhang, Xi Chen, Changgen Feng International Conference on Materials Science, Resource and Environmental Engineering . 2017

机译：新型蛋白酪氨酸磷酸酶1B抑制剂的发现与研究
5. Isolation and partial identification of a polysaccharide from Symphytum officinale L. as a potent inhibitor of protein tyrosine phosphatase 1B (PTP1 B). [D] . Chen, I-Ching Sandy. 2016

机译：从Syphytum officinale L.分离并部分鉴定为蛋白质酪氨酸磷酸酶1B（PTP1 B）的有效抑制剂的多糖。
6. Interaction of Constitutive Photomorphogenesis 1 Protein with Protein-Tyrosine Phosphatase 1B Suppresses Protein-Tyrosine Phosphatase 1B Activity and Enhances Insulin Signaling [O] . Wenying Ren, Yingmin Sun, Sarwat Cheema, 2013

机译：本构光形态发生1蛋白与蛋白酪氨酸磷酸酶1B的相互作用抑制蛋白酪氨酸磷酸酶1B活性并增强胰岛素信号传导。
7. Protein Tyrosine Phosphatase Interacting Protein 51 (PTPIP51) mRNA Expression and Localization and Its In Vitro Interacting Partner Protein Tyrosine Phosphatase 1B (PTP1B) in Human Placenta of the First, Second, and Third Trimester [O] . Stenzinger, Albrecht, Märker, David, Koch, Philipp, 2008

机译：酪氨酸磷酸酶相互作用蛋白51（PTPIP51）mRNA的表达和定位及其在人的妊娠早期，孕中期和孕中期的相互作用伴侣蛋白酪氨酸磷酸酶1B（PTP1B）

Synthesis of novel benzofuran isoxazolines as protein tyrosine phosphatase 1B inhibitors.

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