African Journal of
Pharmacy and Pharmacology

  • Abbreviation: Afr. J. Pharm. Pharmacol.
  • Language: English
  • ISSN: 1996-0816
  • DOI: 10.5897/AJPP
  • Start Year: 2007
  • Published Articles: 2198

Full Length Research Paper

Synthesis and evaluation of chalcone analogues and pyrimidines as cyclooxygenase (COX) inhibitors

Syed Nasir Abbas Bukhari1*, Waqas Ahmad1, Adeel Masood Butt1, Naveed Ahmad1, Muhammad Wahab Bin Amjad1, Muhammad Ajaz Hussain2, Viresh H Shah3 and Amit R Trivedi3
1Faculty of Pharmacy, Universiti Kebangsaan Malaysia, Kuala Lumpur, 50300, Malaysia.  2Department of Chemistry, University of Sargodha, Sargodha, Pakistan. 2Department of Chemistry, Saurashtra University, Rajkot- 360 005, Gujarat, India.
Email: [email protected]

  •  Accepted: 05 March 2012
  •  Published: 15 April 2012

Abstract

A series of chalcone analogues was synthesized and used as precursor for the synthesis of novel series of pyrimidines. Both groups have been evaluated for their effects on the cyclooxygenases (COXs) that are imperative enzymes in the genesis of prostaglandin H2, which is an antecedent for the biosynthesis of prostaglandins, thromboxanes and prostacyclins. The results depicted that chalcones and pyrimidines are very active inhibitors according to the pattern of substitution. Compounds C4, C5, P4 and P5 with methoxylation and nitro substitutions showed best results to inhibit COX-2.

 

Key words: COX inhibitors, chalcones, pyrimidines, anti-inflammatory agents.