Synthesis, anti-inflammatory, antiplatelet and in silico evaluations of (E)-3-(3-(2,3-dihydro-3-methyl-2-oxo3H -benzoxazole-6-yl)-1-phenyl-1H -pyrazole4-yl)acrylamides
Synthesis, anti-inflammatory, antiplatelet and in silico evaluations of (E)-3-(3-(2,3-dihydro-3-methyl-2-oxo- 3H-benzoxazole-6-yl)-1-phenyl-1H-pyrazole- 4-yl)acrylamides
Among the synthesized derivatives 7a--k, especially compound 7g exhibited dual anti-inflammatory and antiplatelet activity with selective COX-2 inhibition.
📌 3 Key Takeaways
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Objective & Hypothesis:A series of (E)-3-(3-(2,3-dihydro-3-methyl-2-oxo-3H-benzoxazole- 6-yl)-1-phenyl-1H-pyrazole-4-yl)acry- lamides (7a--k) were synthesized and evaluated for their in vitro inhibitory activities on COX-1 and COX-2 isoforms using a human whole blood assay as well as their antiplatelet profile against human platelet aggregation using arachidonic acid as agonists.
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Key Findings & Data:A series of (E)-3-(3-(2,3-dihydro-3-methyl-2-oxo-3H-benzoxazole- 6-yl)-1-phenyl-1H-pyrazole-4-yl)acry- lamides (7a--k) were synthesized and evaluated for their in vitro inhibitory activities on COX-1 and COX-2 isoforms using a human whole blood assay as well as their antiplatelet profile against human platelet aggregation using arachidonic acid as agonists.
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Conclusion & Impact:Among the synthesized derivatives 7a--k, especially compound 7g exhibited dual anti-inflammatory and antiplatelet activity with selective COX-2 inhibition.
A series of (E)-3-(3-(2,3-dihydro-3-methyl-2-oxo-3H-benzoxazole- 6-yl)-1-phenyl-1H-pyrazole-4-yl)acry- lamides (7a--k) were synthesized and evaluated for their in vitro inhibitory activities on COX-1 and COX-2 isoforms using a human whole blood assay as well as their antiplatelet profile against human platelet aggregation using arachidonic acid as agonists. Among the synthesized derivatives 7a--k, especially compound 7g exhibited dual anti-inflammatory and antiplatelet activity with selective COX-2 inhibition.
Özet
A series of (E)-3-(3-(2,3-dihydro-3-methyl-2-oxo-3H-benzoxazole- 6-yl)-1-phenyl-1H-pyrazole-4-yl)acry- lamides (7a--k) were synthesized and evaluated for their in vitro inhibitory activities on COX-1 and COX-2 isoforms using a human whole blood assay as well as their antiplatelet profile against human platelet aggregation using arachidonic acid as agonists. Among the synthesized derivatives 7a--k, especially compound 7g exhibited dual anti-inflammatory and antiplatelet activity with selective COX-2 inhibition.
BAYTAŞ, S., DURAL, N. N. T., ÖZKAN, Y. (2012). Synthesis, anti-inflammatory, antiplatelet and in silico evaluations of (E)-3-(3-(2,3-dihydro-3-methyl-2-oxo3H -benzoxazole-6-yl)-1-phenyl-1H -pyrazole4-yl)acrylamides. Turkish Journal of Chemistry, Cilt: 36 - Sayı: 3, 367–382. https://ajindex.com/articles/185263