Friday, October 24, 2014

Nimesulide Synthesis

Nimesulide is a non-steroidal anti-inflammatory drug (NSAID) with analgesic and antipyretic properties which, preferentially inhibits the enzyme cyclooxygenase-2 (COX-2)

It has better gastro-intestinal tolerability among other NSAIDs in its class. Its approved indications are the treatment of acute pain, the symptomatic treatment of osteoarthritis and primary dysmenorrhoea, sports injuries etc.

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) )

Clinically it has proven that it supports a particularly good profile in terms of gastrointestinal tolerability.

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