Pyrazolonees

In medicine, pyrazolonee derivatives play a significant role as analgesics, anti-inflammatory, and fever-reducing agents. Among these are antipyrin, butadion, amidopyrin, phenylpyrazon, sulfinpyrazone, sodium methamizol sodium (analgin), and a few others. In terms of analgesic and anti-inflammatory action, they are similar to salicylic acid derivatives. Although the mechanism of their action is not completely known, it is supposed that pyrazolone derivatives, like aspirin, inhibit biosynthesis of prostaglandins and reduce permeability of capillaries, thus preventing the development of inflammatory reactions. A serious limitation to the wide use of pyrazolonee in medicine is the cases of onset of agran-ulocytosis upon use of methamizol sodium.

Nevertheless, the most widely used derivative in medicine is methamizol sodium (although it is prohibited in some countries) as well as combined drugs on its base; in particular, baralgin, which represents a combined drug based on methamizol sodium with the spasmolytic 4'-(ethoxypiperidine)carbomethoxybenzophenone and the ganglionic blocker 2,2-diphenyl-4-piperidylacetamide.

Phenylbutazone: Phenylbutazone, 4-butyl-1,2-diphenyl-3,5-pyrazolidinedione (3.2.6), is synthesized in a single stage by reacting hydrazobenzol with butylmalonic ester [68,69].

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