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Design, synthesis, biological evaluation, and computational studies of novel thiazolo-pyrazole hybrids as promising selective COX-2 inhibitors: Implementation of apoptotic genes expression for ulcerogenic liability assessment
Faculty
Medicine
Year:
2021
Type of Publication:
ZU Hosted
Pages:
Authors:
Adel Mohamed AbdelKhalek AbouRejaili,
Staff Zu Site
Abstract In Staff Site
Journal:
Bioorganic Chemistry Elsevier
Volume:
Keywords :
Design, synthesis, biological evaluation, , computational studies
Abstract:
A novel series of thiazolo-pyrazole hybrids has been prepared and assessed for their in vitro COX-1/COX-2 inhibitory activity. Compound 6c exhibited the most selective COX-2 inhibition profie (SI of 264) not far of Celecoxib (2 9 4). In-vivo anti-inflmmatory activity revealed that compound 6d exhibited the highest activity (97.30% inhibition of edema) exceeding reference standard Indomethacin (84.62% inhibition of edema). The ulcerogenic liability tested, using gross, microscopic, biochemical analysis and apoptotic genes expression, showed that compound 6b matched the optimal candidate activity (ulcer index = 120, selectivity index of ~ 162 and 77% in-vivo inhibition of edema). Meanwhile, compound 6 m (ulcer index = 0) showcased the highest safety profie. Molecular modeling analysis and drug likeness studies presented appreciated agreement with the biological evaluation
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Department Related Publications
Ashraf Saber Bayoumi Hegab, "التاثير المحسن لفيتامين هـ ضد سمنه على التركيب النسيجى للخصيه والنمط الصبغى في الجرذان البيضاء البالغه ", لايوجد, 1900
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Gamal Mohamed Zain Elabdein, "تكوين الصمام السمعى الظاهر والغشاء الطبلى في الفئران قبل الولادة", لايوجد, 1900
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