Synthesis and biological evaluation of novel ...
|Title||Synthesis and biological evaluation of novel pyrazole compounds.|
|Author(s)||A. Youssef, E. Neeland, E. Villanueva, M. White, I. El-Ashmawy, B. Patrick, A. Klegeris, A. Abd-El-Aziz|
|Journal||Section Title: Pharmacology, Bioorganic & Medicinal Chemistry|
|Abstract||A novel dipyrazole ethandiamide compd. and acid chloride of pyrazolo[3,4-d]pyrimidine 4(5H)-one were prepd. and reacted with a no. of nucleophiles. The resultant novel compds. were tested in several in vitro and in vivo assays. Three compds. inhibited the secretion of neurotoxins by human THP-1 monocytic cells at concns. that were not toxic to these cells. They also partially inhibited both cyclooxygenase-1 and -2 isoforms. In animal studies, two compds. were notable for their anti-inflammatory activity that was comparable to that of the clin. available cyclooxygenase-2 inhibitor celecoxib. Modeling studies by using the mol. operating environment module showed comparable docking scores for the two enantiomers docked in the active site of cyclooxygenase-2. [on SciFinder(R)]|
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