Scholarlink

<p>The cyclooxygenase 1 and 2 (COX-1 and COX-2) are the key enzymes that are responsible for the conversion of arachidonic acid to prostaglandins. Meanwhile, nonsteroidal anti-inflammatory drugs (NSAIDs) are considered as a double-edged weapon to inhibit COX-1 can lead to gastrointestinal side effects and kidney damage, whereas selective COX-2 inhibition provides anti-inflammatory effects without gastrointestinal toxicity. In this report, we described the modular synthesis of substituted pyridazin-3(<i>2H</i>)-ones in polyethylene glycol-400, as a green solvent. The products were isolated without the use of column chromatography, which makes this process elegant and efficient. The compounds <b>2e</b> and <b>2 l</b> show the top-tier selective index for cyclooxygenase, in comparable with celecoxib as a standard. Besides, the antioxidant activity of the synthesized compounds has also been tested. The binding mode of <b>2 h</b> was evaluated through in silico molecular docking, while ADME assessment studies predicted the drug-like characteristics of the synthesised compounds <b>(2a-p).</b> The newly developed protocol and synthesized compounds may serve as a structural guide for designing and development of cyclooxygenase inhibitors.</p> Graphical abstract <p></p>

错误：搜索内容不能为空，请输入英文关键词
错误：关键词超出字数限制，请精简
高级检索

Design and synthesis of pyridazinone hybrid in PEG-400 as COX-1/COX-2 inhibitor and their antioxidant study

  • 期刊论文

  • 出版模式：

    开放获取

  • 发表日期：

    2025年6月15日

查看全文
  • Omprakash B. Pawar,
  • Anil P. Marale,
  • Deekshaputra R. Birhade,
  • Rahul D. Jawarkar,
  • Avinash G. Ulhe,
  • Gajanan D. Rawate,
  • Nagesh R. Nahate,
  • Shashikant A. Ikhe,
  • Dinesh A. Pund,
  • Gajanan N. Chaudhari,
  • Vivek T. Humne

摘要

The cyclooxygenase 1 and 2 (COX-1 and COX-2) are the key enzymes that are responsible for the conversion of arachidonic acid to prostaglandins. Meanwhile, nonsteroidal anti-inflammatory drugs (NSAIDs) are considered as a double-edged weapon to inhibit COX-1 can lead to gastrointestinal side effects and kidney damage, whereas selective COX-2 inhibition provides anti-inflammatory effects without gastrointestinal toxicity. In this report, we described the modular synthesis of substituted pyridazin-3(2H)-ones in polyethylene glycol-400, as a green solvent. The products were isolated without the use of column chromatography, which makes this process elegant and efficient. The compounds 2e and 2 l show the top-tier selective index for cyclooxygenase, in comparable with celecoxib as a standard. Besides, the antioxidant activity of the synthesized compounds has also been tested. The binding mode of 2 h was evaluated through in silico molecular docking, while ADME assessment studies predicted the drug-like characteristics of the synthesised compounds (2a-p). The newly developed protocol and synthesized compounds may serve as a structural guide for designing and development of cyclooxygenase inhibitors.

Graphical abstract