Synthesis and biological evaluation of novel ...

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Title Synthesis and biological evaluation of novel pyrazole compounds.
Author(s) Amal M. Youssef, Edward G. Neeland, Erika B. Villanueva, M. Sydney White, Ibrahim M. El-Ashmawy, Brian Patrick, Andis Klegeris, Alaa S. Abd-El-Aziz
Journal Bioorganic & medicinal chemistry,
Date 2010
Volume 18
Issue 15
Start page 5685
End page 5696
Abstract A novel dipyrazole ethandiamide compound and acid chloride of pyrazolo[3,4-d]pyrimidine 4(5H)-one were prepared and reacted with a number of nucleophiles. The resultant novel compounds were tested in several in vitro and in vivo assays. Three compounds inhibited the secretion of neurotoxins by human THP-1 monocytic cells at concentrations that were not toxic to these cells. They also partially inhibited both cyclooxygenase-1 and -2 isoforms. In animal studies, two compounds were notable for their anti-inflammatory activity that was comparable to that of the clinically available cyclooxygenase-2 inhibitor celecoxib. Modeling studies by using the molecular operating environment module showed comparable docking scores for the two enantiomers docked in the active site of cyclooxygenase-2.
DOI 10.1016/j.bmc.2010.06.018
PubMed ID 20609589

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