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Mohamed LW, El-Badry OM, El-Ansary AK, et al. Design & synthesis of novel oxazolone & triazinone derivatives and their biological evaluation as COX-2 inhibitors. Bioorg Chem. 2017;72:308-314doi: 10.1016/j.bioorg.2017.04.012.
Mohamed, L. W., El-Badry, O. M., El-Ansary, A. K., & Ismael, A. (2017). Design & synthesis of novel oxazolone & triazinone derivatives and their biological evaluation as COX-2 inhibitors. Bioorganic chemistry, 72308-314. https://doi.org/10.1016/j.bioorg.2017.04.012
Mohamed, Lamia W, et al. "Design & synthesis of novel oxazolone & triazinone derivatives and their biological evaluation as COX-2 inhibitors." Bioorganic chemistry vol. 72 (2017): 308-314. doi: https://doi.org/10.1016/j.bioorg.2017.04.012
Mohamed LW, El-Badry OM, El-Ansary AK, Ismael A. Design & synthesis of novel oxazolone & triazinone derivatives and their biological evaluation as COX-2 inhibitors. Bioorg Chem. 2017 Jun;72:308-314. doi: 10.1016/j.bioorg.2017.04.012. Epub 2017 Apr 24. PMID: 28500957.
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Bioorg Chem. 2017 Jun;72:308-314. doi: 10.1016/j.bioorg.2017.04.012. Epub 2017 Apr 24.

Design & synthesis of novel oxazolone & triazinone derivatives and their biological evaluation as COX-2 inhibitors.

Bioorganic chemistry

Lamia W Mohamed, Osama M El-Badry, Afaf K El-Ansary, Ahmed Ismael

Affiliations

  1. Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Cairo University, Cairo 11562, Egypt. Electronic address: [email protected].
  2. Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Cairo University, Cairo 11562, Egypt; Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy Ahram Canadian University, Cairo 11562, Egypt.
  3. Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Cairo University, Cairo 11562, Egypt.
  4. Quality Control Department, Egyptian International Pharmaceutical Industries Co. (EIPICO), Cairo 11562, Egypt.

PMID: 28500957 DOI: 10.1016/j.bioorg.2017.04.012

Abstract

A new series of oxazolones and triazinones were designed and synthesized and evaluated against both COX-1 and COX-2 enzymes. Full structure elucidation of the new derivatives was performed using microanalyses, IR, 1H NMR, 13C NMR and mass spectra. Most of the derivatives showed good inhibitory activity against COX-2 enzyme specifically compounds IIIc, IIIe, IVd and IVg with IC50 values 0.024, 0.019, 0.011 and 0.014µM compared to celecoxib as reference drug with IC50 value of 0.05µM. Altogether, these results indicate that these derivatives can be effective anti-inflammatory agents.

Copyright © 2017 Elsevier Inc. All rights reserved.

Keywords: Anti-inflammatory; Antitumor; COX-1; COX-2; Oxazolone; Synthesis; Triazinone

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