Novel Anti-inflammatory Agents Based on Pyrazole Based Dimeric Compounds; Design, Synthesis, Docking and in Vivo Activity

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概要

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• Series of pyrazole ester prodrugs analogues have been synthesized and found to contain highly potent inhibitors of the cyclooxygenase-2 (COX-2) enzyme. The paper describes synthesis of the target pyrazole analogues. The structure of the synthesized mutual ester prodrugs (6—8c) were confirmed by 1H-, 13C-NMR mass spectroscopy (MS) and their purity were ascertained by TLC and elemental analyses. The biological in vivo evaluation of these compounds in experimental models (carrageenan-induced oedema) proved the presence of anti-inflammatory activity. Docking studies into the catalytic site of COX-2 were used to identify potential anti-inflammatory lead compounds. One lead derivative was chosen endowed with good binding energies.

著者

• Tewari Ashish

  Department of Chemistry, Faculty of Science, Banaras Hindu University

• Srivastava Priyanka

  Department of Chemistry, Faculty of Science, Banaras Hindu University

• Singh Ved

  Department of Chemistry, Faculty of Science, Banaras Hindu University

• Singh Amit

  Department of Pharmacology, IMS, Banaras Hindu University

• Goel Raj

  Department of Pharmacology, IMS, Banaras Hindu University

• Mohan Chethampadi

  Centre for Pharmacoinformatics, National Institute of Pharmaceutical Education and Research (NIPER)

• Mohan Chethampadi

  Centre For Pharmacoinformatics National Inst. Of Pharmaceutical Education And Res. (niper)

• SINGH Amit

  Department of Pharmaceutics, NGSM Institute of Pharmaceutical Sciences

関連論文

• Novel Anti-inflammatory Agents Based on Pyrazole Based Dimeric Compounds; Design, Synthesis, Docking and in Vivo Activity
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