Discovery of 1,3-diphenyl-1H-pyrazole derivatives containing rhodanine-3-alkanoic acid groups as potential PTP1B inhibitors

Sun Liangpeng; Wang Peipei; Xu Lili; Gao Lixin; Li Jia; Piao Huri

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Discovery of 1,3-diphenyl-1H-pyrazole derivatives containing rhodanine-3-alkanoic acid groups as potential PTP1B inhibitors

机译：发现1,3-二苯基-1H-吡唑衍生物，含有罗丹宁-3-链烷酸组作为潜在的PTP1B抑制剂

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摘要

Two series of 1,3-diphenyl-1H-pyrazole derivatives containing rhodanine-3-alkanoic acid groups were identified as competitive protein tyrosine phosphatase 1B (PTP1B) inhibitors. Among the compounds studied, IIIv was found to have the best in vitro inhibition activity against PTP1B (IC50 = 0.67 +/- 0.09 mu M) and the best selectivity (9-fold) between PTP1B and T-cell protein tyrosine phosphatase (TCPTP). Molecular docking studies demonstrated that compounds IIIm, IIIv and IVg could occupy simultaneously at both the catalytic site and the adjacent pTyr binding site. These results provide novel lead compounds for the design of inhibitors of PTP1B as well as other PTPs.

机译：含有氟硝基-3-链烷酸基团的两种1,3-二苯基-1H-吡唑衍生物被鉴定为竞争性蛋白酪氨酸磷酸酶1B（PTP1B）抑制剂。在研究的化合物中，IIIV被发现对PTP1B（IC50 = 0.67 +/-0.09μm）具有最佳的体外抑制活性，并且PTP1b和T细胞蛋白酪氨酸磷酸酶（TCPTP）之间的最佳选择性（9倍）。分子对接研究表明，化合物IIIM，IIIV和IVG可以在催化位点和相邻的PTYR结合位点同时占用。这些结果提供了用于设计PTP1B抑制剂以及其他PTP的新型铅化合物。

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来源
《Bioorganic and Medicinal Chemistry Letters》 |2019年第10期|共7页
作者
Sun Liangpeng; Wang Peipei; Xu Lili; Gao Lixin; Li Jia; Piao Huri;
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作者单位

Yanbian Univ Coll Med Yanji 133000 Peoples R China;

Chinese Acad Sci Natl Ctr Drug Screening Shanghai Inst Mat Med Shanghai Inst Biol Sci Shanghai;

Yanbian Univ Key Lab Nat Resources Changbai Mt &

Funct Mol Minist Educ Coll Pharm Yanji 133000;

Chinese Acad Sci Natl Ctr Drug Screening Shanghai Inst Mat Med Shanghai Inst Biol Sci Shanghai;

Chinese Acad Sci Natl Ctr Drug Screening Shanghai Inst Mat Med Shanghai Inst Biol Sci Shanghai;

Yanbian Univ Key Lab Nat Resources Changbai Mt &

Funct Mol Minist Educ Coll Pharm Yanji 133000;

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原文格式 PDF
正文语种 eng
中图分类药学;
关键词
PTP1B inhibitor; 1; 3-Diphenyl-1H-pyrazole; Rhodanine-3-alkanoic acid;

机译：PTP1B抑制剂;1;3-二苯基-1H-吡唑;罗丹宁-3-链烷酸;

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专利

1. Discovery of 1,3-diphenyl-1H-pyrazole derivatives containing rhodanine-3-alkanoic acid groups as potential PTP1B inhibitors [J] . Sun Liangpeng, Wang Peipei, Xu Lili, Bioorganic and Medicinal Chemistry Letters . 2019,第10期

机译：发现1,3-二苯基-1H-吡唑衍生物，含有罗丹宁-3-链烷酸组作为潜在的PTP1B抑制剂
2. Mono- and disalicylic acid derivatives: PTP1B inhibitors as potential anti-obesity drugs [J] . Suja Shrestha, Bharat Raj Bhattarai, Keun-Hyeung Lee, Bioorganic and Medicinal Chemistry . 2007,第20期

机译：单和二水杨酸衍生物：PTP1B抑制剂可作为潜在的抗肥胖药
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机译：（（3-溴-7-氰基-2-萘基）（二氟）甲基）膦酸，有效和口服活性小分子PTP1B抑制剂的发现。
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机译：聚（乳酸）和乳酸衍生物的技术和经济潜力

Discovery of 1,3-diphenyl-1H-pyrazole derivatives containing rhodanine-3-alkanoic acid groups as potential PTP1B inhibitors

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