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2 Polish Journal of Chemical Technology

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Synthesis, characterization, and molecular modeling of novel 1,3,4-oxadiazole derivatives of mefenamic acid

Bhat Mashooq A., Naglah Ahmed M., Bakheit Ahmed Hassan, Al-Omar Mohamad A.

Polish Journal of Chemical Technology

2024

Vol. 26, nr 1

102--112

A novel series of 1,3,4-oxadiazole derivatives of mefenamic acid was obtained by reacting hydrazones of mefenamic acid with anhydrous acetic anhydride. The mefenamic hydrazones were obtained by reacting different substituted aldehydes with mefenamic acid hydrazide. All the compounds were characterized by spectral data and elemental analysis. Molecular docking studies of all the compounds were performed against COX-1/COX-2 enzymes. Compound 4 and compound 10 were found to have the highest potential to bind with COX-1 while compound 3, compound 6, and compound 10 were found to have the highest potential to bind with COX-2 enzyme.

Facile synthesis and anticancer activity of novel dihydropyrimidinone derivatives

Bhat Mashooq A., Al-Omar Mohamed A., Naglah Ahmed M., Al-Dhfyan Abdullah

Polish Journal of Chemical Technology

2022

Vol. 24, nr 1

23--28

The enaminone, (2E)-3-(dimethylamino)-1-(3,4,5-trimethoxyphenyl) prop-2-en-1-one was prepared by refluxing 3,4,5-trimethoxy acetophenone with dimethylformamide dimethylacetal (DMF–DMA) without solvent for 12 h. The dihydropyrimidinone derivatives (1–9) were prepared by reacting enaminone, substituted benzaldehydes and urea in glacial acetic acid. The compounds (1–9) were synthesized in significant yield using one step multicomponent reaction. Structures of all the novel synthesized compounds were characterized and confirmed by various spectroscopic methods. The compounds were evaluated for their anti-cancer activity against HepG2 cancer cell line. Compound 9 displayed significant anti-cancer activity. During the apoptotic assay, it showed a significant increase in necrosis from 1.97% to 12.18% as compared to the control. Mechanism of anti-proliferation was performed by cell cycle distribution assay, which showed a decrease in G2+M from 12.90 to 8.13 as compared to control.