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Synthesis and biological evaluation of novel pyrazole compounds |
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| Authors: | 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 |
| Affiliation: | 1. Department of Chemistry, University of British Columbia Okanagan, Kelowna, BC, Canada;2. Department of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Alexandria, Alexandria, Egypt;3. Department of Biology, University of British Columbia Okanagan, Kelowna, BC, Canada;4. Department of Pharmacology, Faculty of Veterinary Medicine, University of Alexandria, Alexandria, Egypt;5. X-ray Facility, University of British Columbia Vancouver, BC, Canada |
| 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. |
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