Synthesis and biological evaluation of novel ...



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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