Close Menu

Books in a Library

Pharmacological Evaluation of Marginally Designed New Profen Analogues



Objective: Pharmacological evaluate of hydrazide, marginal analogues of naproxen, flurbiprofen and ibuprofen, well established COX inhibitors, with the goal to identifying a Cyclooxygenase (COX) inhibitor(s) with optimum potency and efficacy. The synthesized and characterized analogues were tested for their acute toxicity, anti-inflammatory, analgesic and antipyretic activities as per reported models. Molecular docking analysis was also performed to predict ligand: protein interactions.

Method: Acute toxicity, anti-inflammatory, analgesic and antipyretic activities were performed in accordance with well-established reported bioassay models for the purposes.

Results: No acute toxicity was observed at intraperitoneal doses of 50, 100 and 150mg/Kg body weight. Biological assays revealed that test compounds -I to -IV have highly significant anti-inflammatory and peripheral analgesic activities. Antipyretic test revealed that test compounds I, II, III have highly significant antipyretic activity while IV in the doses of 20mg and 30 mg has significant and in the dose of 50 mg/Kb body weight has highly significant antipyretic activity. The molecular modelling revealed strong inhibitory interactions of the four compounds. The most suitable poses have higher docking score (energies) compared to flurbiprofen (reference ligand), that confirms highly significant anti-inflammatory and analgesic activities of the dimers.

Conclusion: The synthesized dimerized analogues have highly significant pharmacological activities and have the potential to be further explored as new drug molecules.

13 Feb, 2017
PDF Attachment: 
e-Published: 02 Mar, 2017


Manuscripts that are Published Ahead of Print have been peer reviewed and accepted for publication by the Editorial Board of the West Indian Medical Journal. They may appear in their original format and may not be copy edited or formatted in the style guide of this Journal. While accepted manuscripts are not yet assigned a volume, issue or page numbers, they can be cited using the DOI and date of e-publication. See our Instructions for Authors on how to properly cite manuscripts at this stage. The contents of the manuscript may change before it is published in its final form. Manuscripts in this section will be removed once they have been issued to a volume and issue, but will still retain the DOI and date of e-publication.

Top of Page