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Synthesis, molecular docking and anti-inflammatory screening of novel quinoline incorporated pyrazole derivatives using the Pfitzinger reaction II.

Authors
  • El-Feky, Said A H1
  • Abd El-Samii, Zakaria K2
  • Osman, Nermine A2
  • Lashine, Jasmine2
  • Kamel, Mohamed A3
  • Thabet, Hamdy Kh4
  • 1 Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Northern Border University, PO Box 840, Rafha 91911, Saudi Arabia; Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy, Zagazig University, Zagazig, Egypt. Electronic address: [email protected] , (Egypt)
  • 2 Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy, Zagazig University, Zagazig, Egypt. , (Egypt)
  • 3 Department of Pharmacology, Faculty of Veterinary Medicine, Zagazig University, Zagazig, Egypt. , (Egypt)
  • 4 Department of Chemistry, Faculty of Arts and Science, Northern Border University, PO Box 840, Rafha 91911, Saudi Arabia; Department of Chemistry, Faculty of Science, Al-Azhar University, Nasr City, Cairo 11284, Egypt. , (Egypt)
Type
Published Article
Journal
Bioorganic chemistry
Publication Date
Feb 01, 2015
Volume
58
Pages
104–116
Identifiers
DOI: 10.1016/j.bioorg.2014.12.003
PMID: 25590381
Source
Medline
Keywords
License
Unknown

Abstract

In continuation of our study of novel quinolines with anti-inflammatory activity using the Pfitzinger reaction, several new quinoline derivatives were synthesized and tested for their anti-inflammatory and ulcerogenic effect. A docking study on the COX-2 binding pocket was carried out for the target compounds to rationalize the possible selectivity of them against COX-2 enzyme. The most active compounds (5a, 8a and 11a) were found to be superior to celecoxib. Compound 11a demonstrated the highest anti-inflammatory activity as well as the best binding profiles into the COX-2 binding site. Moreover, compounds 9c, 9e, 10a and 11a were devoid of ulcerogenic activity.

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