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.
Originalsprog | Engelsk |
---|---|
Tidsskrift | Bioorganic & Medicinal Chemistry |
Vol/bind | 18 |
Udgave nummer | 15 |
Sider (fra-til) | 5685-96 |
Antal sider | 12 |
ISSN | 0968-0896 |
DOI | |
Status | Udgivet - 1 aug. 2010 |
Udgivet eksternt | Ja |