Synthesis and in-silico studies of some diaryltriazole derivatives as potential cyclooxygenase inhibitors

被引:0
|
作者
Awwad A. Radwan
Kamal E. H. elTahir
机构
[1] Kayyali’s Chair,Department of Pharmaceutical Organic Chemistry
[2] College of Pharmacy,Department of Pharmacology
[3] King Saud University,undefined
[4] Faculty of Pharmacy,undefined
[5] Assiut University,undefined
[6] College of Pharmacy,undefined
[7] King Saud University,undefined
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关键词
Triazole; Cyclooxygenase; Antiinflammatory; Surflex-Dock;
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摘要
The synthesis of several 4-phenyl-5-pyridin-4-yl-2,3-dihydro-3H-1,2,4-triazole-3-thiones possessing N-2 Mannich bases or S-alkyl substituents, is reported. Several of them exhibited a low nanomolar COX enzyme inhibition activity. Most of the compounds showed inhibition of edema was similar to that evoked by celocoxib in animal model. Molecular docking studies of the compounds into the binding sites of COX-1 and COX-2 allowed us to shed light on the binding mode of these novel COX inhibitors.
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页码:553 / 563
页数:10
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