الفهرس 
IntroductionOnly 14 pages are availabe for public view
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Abstract
Among the most broadly used therapeutics are Non-steroidal anti-inflammatory drugs (NSAIDs), although their amplification is limited because of their adverse effects related to the GIT. NSAIDs exhibit its biological activity through the inhibition of cyclooxygenase (COX) enzyme, which has two main isoforms COX-1 isoform and COX-2 isoform. COX-2 isoform is the one believed to be related to inflammation. So,based on SAR study for the known selective COX-2 inhibitors, our aim to design and synthesis A novel series of 2-Benzamido-N-(4- substitutedphenyl)thiophene-3-carboxamide derivatives as selective COX-2 inhibitors through modification of diclofenac structure. Their biological activity is evaluated as anti-inflammatory with assaying their IC50 and compared with celecoxib.Compound 2-benzamido-5-ethyl-N-(4-fluorophenyl)thiophene-3-carboxamide (VIIa) shows high anti-inflammatory activity with IC50 0.29 and selectivity index 67.24 twice of celecoxib. Molecular docking studies for compound (VIIa) show high binding affinity toward COX-2. Bioinformatics studied for compound (VIIa) show promising drug-like properties. Nano drug delivery system of compound (VIIa) is prepared to enhance its releasing profile which is matter of concern in chronic treatment as in case of chronic inflammation.