Tuesday, January 27, 2015

Nimesulide Tablet Synthesis

Nimesulide is a non-steroidal anti-inflammatory agent that is generally utilized as a part of the treatment of inflammatory torment which hinders the protein cyclooxygenase-2 (COX-2) and has better gastro-intestinal mediocrity in addition to different NSAIDs in its class.

Its approved signs are the treatment of intense torment, the symptomatic treatment of osteoarthritis and essential dysmenorrhoea, sports wounds and so on.

A variety of new Nimesulide derivatives were synthesized through incorporation of a 5-LOX pharmacophore into nimesulide followed with some structural modifications, which were then characterized for dual enzyme inhibitors for these two types of enzymes (Cyclooxygenase-½ (COX-½) and 5-lipoxygenase (5-LOX) ). Their structure-activity relationships (SARs) were studied, and compound 20f was found to be an excellent dual enzyme inhibitor.

Its binding conformation and interaction mode were studied with molecular docking experiments. Compound 20f could become a lead compound for further development for potential anti-inflammatory drugs.

Clinically it has demonstrated that it supports an especially good profile as far as gastrointestinal tolerability.

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