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N4-Amino-acid derivatives of 6-azacytidine: Structure-activity relationship.

100%
Alexeeva I., Palchikovskaya L., Shalamay A., Nosach L., Zhovnovataya V., Povnitsa O., Dyachenko N.
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2000
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vol. 47
|
issue 1
95-101
EN
Several N4-derivatives of 6-azacytidine were synthesized using of Vorbrüggen's condensation method. Their antiviral activity with respect to the adenovirus serotypes 2 and 5 in Hep-2 cells culture was studied and primary specific activity was determined. Correlation between chemical structure of new 6-azacytidine derivatives and their biological properties is discussed.
2
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Antiviral activity of novel oseltamivir derivatives against some influenza virus strains

88%
Kocik J., Kołodziej M., Joniec J., Kwiatek M., Bartoszcze M.
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2014
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vol. 61
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issue 3
509-513
EN
The aim of this study was to investigate the in vitro cytotoxicity of oseltamivir derivatives and determine their activity against A/H1N1/PR/8/34 and A/H3N2/HongKong/8/68 - strains of influenza virus. Antiviral activity of these compounds was determined by using two methods. MTT staining was used to assess the viability of MDCK cells infected with influenza viruses and treated with various concentrations of drugs. In parallel, the effect of drugs on viral replication was assessed using the hemagglutination test. The most toxic compounds were: OS-64, OS-35, OS-29, OS-27 and OS-25, whereas OS-11, OS-20 and OS-23 were the least toxic ones. Statistically significant antiviral effect at a higher virus dose was shown by compounds: OS-11, OS-20, OS-27, OS-35, and OS-64. H3N2 virus was sensitive to 10-times lower concentrations of OS-11 and OS-35 than H1N1. At a lower infection dose, the antiviral activity was observed for OS-11, OS 27, OS-35 and OS-20. OS-64 turned out to be effective only at a high concentration. OS-23 showed no antiviral effect.
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SYNTHESIS, REACTIONS, AND APPLICATIONS OF HYDANTOIN AND 2-THIOHYDANTOIN DERIVATIVES

75%
Abd Elhady H., El Desoky S., Al-Shareef H. F., El-mekawy R.
Acta Poloniae Pharmaceutica - Drug Research
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2019
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vol. 76
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issue 6
971-986
EN
On account of the interesting pharmacological properties of hydantoin and 2-thiohydantoin derivatives, and other purposes such as textile printing, catalysts for polymerizations, their use in the production of resins and plastics, they have been the subject of chemical and biological studies. In this review article, we focused our interest on the most important methods for the synthesis of hydantoin and 2-thiohydantoin derivatives, different reactions and different application of them. We explored their antitumor, antimicrobial, antiviral, anxiolytic, antidiabetic, anticonvulsant activities, their utilities in treatment of vascular dysfunction, using them as an inhibitor of fatty acid amide hydrolase, using in hyperpigmentation applications, and utilities of them in the production of antimicrobial polyurethane coatings.
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