3-Trifluoromethylpyrazolones derived nucleosides: Synthesis and antiviral evaluation
Dengue (DENV) viral infection is a global public health problem that infrequently develops life threatening diseases such as dengue hemorrhagic fever (DFS) and dengue shock syndrome (DSS). Middle East respiratory syndrome coronavirus (MERS-CoV) is a highly pathogenic human corona virus with 38% fatality rate of infected patients. A series of 4-arylhydrazono-5-trifluoromethyl-pyrazolones, their ribofuranosyl, and 5′-deoxyribofuranosyl nucleosides were synthesized, geometry optimized using Density functional theory (DFT), and evaluated for their antiviral activity. 2-Nitrophenylhydrazonopyra-zolone derivative 5 showed significant activity against MERS-CoV (EC50 = 4.6 μM). The nucleoside analog 8 showed moderate activity against DENV-2 (EC50 = 10 μM), while the activity was abolished with the corresponding 5′-deoxyribonucleoside analogs. The identified hits in this study set this category of compounds for further future optimizations.
Ahmed, Ayman M. S.,Abou-Elkhair, Reham A. I.,El-Torky, Alaa M.,Hassan, Abdalla E. A.
Synthesis and antitumor activity of 5-trifluoromethyl-2,4-dihydropyrazol-3- one nucleosides
2,4-Dihydropyrazole glucosides 3a-3c were prepared and tested for their antitumor activity. The structures of these compounds were established by 1H and 13C-NMR spectroscopy. Glucoside 3b shows an in vitro IC50 value of 16.4 μM against proliferation of the human promyelotic leukemia (HL60) cell line.
Abdou, Ibrahim M.,Saleh, Ayman M.,Zohdi, Hussein F.