Chemical Biology and Drug Design
Chemical Biology and Drug Design
5 years ago

Screening of curcumin derived isoxazole, pyrazoles and pyrimidines for their anti-inflammatory, antinociceptive and cyclooxygenase-2 inhibition

Screening of curcumin derived isoxazole, pyrazoles and pyrimidines for their anti-inflammatory, antinociceptive and cyclooxygenase-2 inhibition
Muhammad Abdul Qadir, Abdul Hameed, Mahmood Ahmed, Muhammad Imran, Muhammad Muddassar
Curcumin has shown pharmacological properties against different phenotypes of various disease models. Different synthetic routes have been employed to develop its numerous derivatives for diverse and improved therapeutic roles. In present study, we have synthesized curcumin derivatives containing isoxazole, pyrazoles and pyrimidines then the synthesized molecules were evaluated for their anti-inflammatory and antinociceptive activities in experimental animal models. Acute toxicity of synthesized molecules was evaluated in albino mice by oral administration. Any behavioral and neurological changes were observed at dose of 10 mg/kg body weight. Additionally, cyclooxygenase-2 (COX-2) enzyme inhibition studies were performed through in-vitro assays. In vivo anti-inflammatory studies showed that curcumin with pyrimidines were most potent anti-inflammatory agents which inhibited induced edema from 74.7-75.9%. Compound 7, 9 and 12 exhibited relatively higher prevention of writhing episodes than any other compound with antinociceptive activity of 73.2, 74.9 and 71.8% respectively. This was better than diclofenac sodium (reference drug, 67.1% inhibition). Similarly COX-2 in vitro inhibition assays results revealed that compound 12 (75.3% inhibition) was the most potent compound. Molecular docking studies of 10, 11 and 12 compounds in human COX-2 binding site revealed the similar binding mode as that of other COX-2 selective inhibitors. This article is protected by copyright. All rights reserved. Guanidine conjugated with curcumin showed excellent COX-2 inhibition (75.3 % inhibition at 10 µM)

Publisher URL: http://onlinelibrary.wiley.com/resolve/doi

DOI: 10.1111/cbdd.13076

You might also like
Discover & Discuss Important Research

Keeping up-to-date with research can feel impossible, with papers being published faster than you'll ever be able to read them. That's where Researcher comes in: we're simplifying discovery and making important discussions happen. With over 19,000 sources, including peer-reviewed journals, preprints, blogs, universities, podcasts and Live events across 10 research areas, you'll never miss what's important to you. It's like social media, but better. Oh, and we should mention - it's free.

  • Download from Google Play
  • Download from App Store
  • Download from AppInChina

Researcher displays publicly available abstracts and doesn’t host any full article content. If the content is open access, we will direct clicks from the abstracts to the publisher website and display the PDF copy on our platform. Clicks to view the full text will be directed to the publisher website, where only users with subscriptions or access through their institution are able to view the full article.