Synthesis and biological evaluation of benzodioxol derivatives as cyclooxygenase inhibitors‏
Publication Type
Original research
Authors

Non-steroidal anti-inflammatory drugs (NSAIDs) are among the most widely used therapeutics; they are competitive inhibitors of cyclooxygenase (COX), the enzyme which mediates the conversion of arachidonic acid to inflammatory prostaglandins.

Objective:

In this study, new benzodioxol derivatives with different core cycles and functional groups (i.e., aryl acetate, aryl acetic acid and diazepine) were designed, synthesized, identified and evaluated for their analgesic and anti-inflammatory activity, as a preliminary screening study to identify the most potent and more selective groups.

Methods:

The synthesized compounds were identified using FTIR, HRMS, 1H-NMR and 13C-NMR, and evaluated for their inhibitory activity against ovine COX-1 and COX-2 using an in vitro cyclooxygenase (COX) inhibition assay kit.

Results and Discussion:

Six compounds were synthesized as a preliminary screening …

Journal
Title
Letters in Drug Design & Discovery
Publisher
Bentham Science Publisher
Publisher Country
United Arab Emirates
Indexing
Thomson Reuters
Impact Factor
1.1
Publication Type
Online only
Volume
17
Year
2020
Pages
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