Silica catalyzed one pot synthesis of hybrid thiazolidin-4- one derivatives as anti-tubercular and anti-inflammatory agent by attenuating COX-2 pathway

Prateek Pathak; Parjanya Kumar Shukla; Vladislav Naumovich; Maria Grishina; Vladimir Potemkin; Amita Verma

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Silica catalyzed one pot synthesis of hybrid thiazolidin-4- one derivatives as anti-tubercular and anti-inflammatory agent by attenuating COX-2 pathway

机译：二氧化硅通过衰减COX-2途径催化杂交噻唑烷-4-4-一种抗结核和抗炎剂的一个罐合成溶液

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A novel series of a hybrid class of hybrid thiazolidin-4-one derivatives were designed and synthesized through one-pot catalytic synthesis. The reaction was catalyzed in the presence of silica-H_2SO4~((+6)). The derivatives computational ADMET profile was calculated. The study shows that most active derivatives have optimal logP, higher anti-inflammatory activity score, and poor metabolism at the sight of P450-3A4 and 2D6. The entire series of derivatives were further evaluated for anti-tubercular (against Mycobacterium tuberculosis H37Rv (Resistant strain)) and antiinflammatory activity (in-vivo assay using Wistar rat). The result showed that derivatives 4c, 4h, and 4m have significant potency against tested M. tuberculosis. However, derivatives 4i and 4j found significantly active against inflammation. In vitro COX inhibition assay also supported the result in favor of selectivity and efficacy of derivatives.

机译：通过单罐催化合成设计并合成了一种新的杂种杂交类杂种杂交类杂交类杂交类衍生物。在二氧化硅-H_2SO4〜（（+ 6））存在下催化反应。计算衍生品计算备用探索。该研究表明，大多数活性衍生物具有最佳的LOMP，抗炎活动评分较高，并且在P450-3A4和2D6的视线中的代谢差。进一步评估整个系列的衍生物，用于抗结核（针对结核分枝杆菌H37RV（抗性菌株））和抗炎活性（使用Wistar RAT的体内测定）。结果表明，衍生物4C，4H和4M和4M具有显着的效力，免受测试的M.结核病。然而，衍生物4i和4J发现显着激活炎症。体外Cox抑制测定也支持衍生物的选择性和功效的结果。

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来源
《Synthetic Communications》 |2019年第20期|共35页
作者
Prateek Pathak; Parjanya Kumar Shukla; Vladislav Naumovich; Maria Grishina; Vladimir Potemkin; Amita Verma;
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作者单位

Laboratory of Modeling of Drugs Higher Medical and Biological School South Ural State University Chelyabinsk Russia;

Bioorganic and Medicinal Chemistry Research Laboratory Department of Pharmaceutical Sciences Faculty of Health Sciences Sam Higginbottom University of Agriculture Technology and Sciences Allahabad India;

Laboratory of Modeling of Drugs Higher Medical and Biological School South Ural State University Chelyabinsk Russia;

Laboratory of Modeling of Drugs Higher Medical and Biological School South Ural State University Chelyabinsk Russia;

Laboratory of Modeling of Drugs Higher Medical and Biological School South Ural State University Chelyabinsk Russia;

Bioorganic and Medicinal Chemistry Research Laboratory Department of Pharmaceutical Sciences Faculty of Health Sciences Sam Higginbottom University of Agriculture Technology and Sciences Allahabad India;

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原文格式 PDF
正文语种 eng
中图分类有机化学;
关键词
ADME; anti-inflammatory activity; docking; thiadiazole; thiazolidine- 4-one;

机译：Adme;抗炎活动;对接;噻唑;噻唑胺 - 4-一;

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1. Silica catalyzed one pot synthesis of hybrid thiazolidin-4- one derivatives as anti-tubercular and anti-inflammatory agent by attenuating COX-2 pathway [J] . Prateek Pathak, Parjanya Kumar Shukla, Vladislav Naumovich, Synthetic Communications . 2019,第17a20期

机译：二氧化硅通过衰减COX-2途径催化杂交噻唑烷-4-4-一种抗结核和抗炎剂的一个罐合成溶液
2. Silica catalyzed one pot synthesis of hybrid thiazolidin-4-one derivatives as anti-tubercular and anti-inflammatory agent by attenuating COX-2 pathway [J] . Pathak Prateek, Shukla Parjanya Kumar, Naumovich Vladislav, Synthetic Communications . 2019,第17a20期

机译：二氧化硅通过衰减COX-2途径催化一个杂交噻唑烷-4-一衍生物作为抗结核和抗炎剂的罐合成
3. Molecular hybrid design, synthesis and biological evaluation of N-phenyl sulfonamide linked N-acyl hydrazone derivatives functioning as COX-2 inhibitors: new anti-inflammatory, anti-oxidant and anti-bacterial agents [J] . Gorantla Vasubabu, Gundla Rambabu, Jadav Surender Singh, New Journal of Chemistry . 2017,第22期

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4. Silica Nanoparticles from Rice Husk Ash: A Green Catalyst for the One-Pot Three- Component Synthesis of BenzoSFuran Derivatives [C] . AN Ramazani, Morteza Rouhani, Sang Woo Joo International Conference on Advanced Material and Manufacturing Science . 2014

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Silica catalyzed one pot synthesis of hybrid thiazolidin-4- one derivatives as anti-tubercular and anti-inflammatory agent by attenuating COX-2 pathway

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