Abstract
In search of novel effective potent therapeutic agents delivered by oral route for inflammation treatment, some novel O-propargylated-N-acetylpyrazole analogs (5a–j) were prepared by treating N-acetylpyrazole (4a–j) derived from 1,3-diarylpropenones (3a–j) with propargyl bromide. Claisen-Schmidt condensation of a series of substituted aryl ketones 1 and benzaldehydes 2 in glacial acetic acid afforded 1,3-diarylpropenones which on further treatment with hydrazine hydrate in acetic acid under reflux conditions afforded 1-acetyl-3,5-diaryl-4,5-dihydro(1H)pyrazoles (4a–j). The products were characterized by using spectroscopic techniques such as IR and NMR. In addition, the in vivo anti-inflammatory activity of the synthesized compounds was determined using the carrageenan-induced paw oedema method in rats.
Highlights
Inflammation is a protective attempt by the organism to remove the injurious stimuli and to initiate the healing process
Current approaches to overcome the inflammation include the use of nonsteroidal anti-inflammatory drugs (NSAIDS), immune selective antiinflammatory derivatives, selective glucocorticoid receptor agonist, resolvins/protectins, and TNF inhibitors
We describe the synthesis of some substituted N-acetylpyrazoles (4a–j) and their corresponding O-propargylate analogs (5a– j) as potent anti-inflammatory agents
Summary
Inflammation is a protective attempt by the organism to remove the injurious stimuli and to initiate the healing process. Drug treatment has been improved to some extent yet, it is still a challenge for the pharmaceutical chemists to explore the more effective and potent therapeutic agents to treat inflammation and reduce the signs and symptoms of acute inflammation and chronic inflammatory diseases. It is well evident from the literature and numerous studies that there is requirement for appropriate modification of the molecules to attenuate the effective potent therapeutic agents for the treatment of inflammation and ensure that the host immune defense against infection is not impaired [1]
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