Synthesis and pharmacological evaluation of amide conjugates of NSAIDs with L -cysteine ethyl ester, combining potent antiinflammatory and antioxidant properties with significantly reduced gastrointestinal toxicity

Synthesis, Anti-Inflammatory Activity, and In Silico Study of Novel Diclofenac and Isatin Conjugates

“…Comprehensive literature survey revealed that Isatin moiety possesses diverse pharmacological activities including anti-inflammatory activity [9–11]. Further, it has been reported that the substituents at the 2- or 3-position of the indole nucleus are closely related to their anti-inflammatory properties [12–14]. The size of active site in cyclooxygenase enzyme COX-2 is larger than cyclooxygenase enzyme COX-1; hence the extension in ligand size may increase the selectivity toward COX-2 enzyme [15].…”

Synthesis and Pharmacological Evaluation of Novel Conjugates of Indomethacin with Antioxidant Activity

“…Recently, some other new conjugates of NSAIDs with L-cysteine ethyl ester, another antioxidant molecule, were synthesized by Kourounakis group, and these derivatives showed potent antiinflammatory activity and considerably reduced gastrointestinal toxicity. 8 Therefore it would be interesting to design compounds with a potential combination of classical antiinflammatory property and antioxidant activity for enhanced antiinflammatory activity as well as reduced ulcerogenic potency. 6 Here, we report the synthesis of some new conjugates of indomethacin with natural phenolic antioxidants and also evaluation of their antioxidant and antiinflammatory activities.…”

Design, synthesis and pharmacological evaluation of novel azole derivatives of aryl acetic acid as anti-inflammatory and analgesic agents

“…Therefore the development of novel compounds having anti-inflammatory and analgesic activity with an improved safety profile is still a necessity. Studies have shown that derivatisation of the carboxylate function of arylalkonic acids resulted in a retained anti-inflammatory activity and reduced ulcerogenic potential [10][11][12][13]. Furthermore it has been reported in the literature that the substituted azole derivatives such as 1,3,4-oxadiazole/thiadiazole [14,15] and 1,2,4 triazole [16] possess significant anti-inflammatory activity.…”