Synthesis and Evaluation: Chalcone Analogues and Pyrimidines as Cyclooxygenase

African Journal of Pharmacy and Pharmacology Vol. 6(14), pp. 1064 - 1068, 15 April, 2012 Available online at http://www.academicjournals.org/AJPP DOI: 10.5897/AJPP12.022 ISSN 1996-0816 ©2012 Academic Journals

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
1

Faculty of Pharmacy, Universiti Kebangsaan Malaysia, Kuala Lumpur, 50300, Malaysia. 2 Department of Chemistry, University of Sargodha, Sargodha, Pakistan. 2 Department of Chemistry, Saurashtra University, Rajkot- 360 005, Gujarat, India.
Accepted 5 March, 2012

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. INTRODUCTION Cyclooxygenases (COXs) are imperative enzymes in the genesis of prostaglandin H2 which is an antecedent for the biosynthesis of prostaglandins, thromboxanes, and prostacyclins (Hamberg et al., 1974). There are two isoforms of COX enzymes: Cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2) correspondingly (Fu et al., 1990). The foremost tasks assigned to COX-1 enzyme include the defence of gastric mucosa, platelet aggregation, and renal blood flow while the COX-2 enzyme is inferable and articulated during inflammation, ache and

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