Synthesis and biological evaluation of novel pyrazole compounds
Research output: Contribution to journal › Journal article › Research › peer-review
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.
Original language | English |
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Journal | Bioorganic & Medicinal Chemistry |
Volume | 18 |
Issue number | 15 |
Pages (from-to) | 5685-96 |
Number of pages | 12 |
ISSN | 0968-0896 |
DOIs | |
Publication status | Published - 1 Aug 2010 |
Externally published | Yes |
Bibliographical note
Copyright (c) 2010 Elsevier Ltd. All rights reserved.
- Anti-Inflammatory Agents/chemical synthesis, Binding Sites, Catalytic Domain, Celecoxib, Cell Line, Computer Simulation, Crystallography, X-Ray, Cyclooxygenase 1/chemistry, Cyclooxygenase 2/chemistry, Cyclooxygenase 2 Inhibitors/chemistry, Humans, Models, Molecular, Pyrazoles/chemical synthesis, Sulfonamides/chemistry
Research areas
ID: 236609943