Inflammation and related disorders are highly prevalent and affect millions of people every year. Inflammation, a complex, biological and defensive response to harmful stimuli or irritants, is often associated with other pathological processes, including Alzheimer's and Parkinson's disease, many cancers and atherosclerosis. Cyclooxygenase-2 (COX-2) is expressed during inflammatory conditions and is responsible for the biosynthesis of the prostaglandins (PGs) required by inflammatory cells. Quantification of COX-2 expression in the brain could potentially be useful for the diagnosis and monitoring of disease progression, as well as a measure of efficacious treatment. To date, no suitable yet specific probe for imaging COX-2 expression has emerged. On this premise, our aim was to develop an optimal probe to provide images of COX-2 expression in the brain. Thus, a series of 1,5-diarylpyrazoles were prepared and evaluated in vitro for their ability to block the activity of the cyclooxygenase-1 and -2 (COX-1 and -2) enzymes.

Preparation and evaluation of new 1,5-diarylpyrazoles as potential probes for imaging cyclooxygenase-2 (COX-2) expression in the brain

244th National Meeting (2012)

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