Abstract
A series of derivatives of 5-hydroxyalkylamino-1,3-oxazoles were synthesized. Among these derivatives, 5 compounds have been evaluated for their activities against a normal laboratory human cytomegalovirus (HCMV) strain, AD169, in human foreskin fibroblast (HFF) cells. Bioassays showed that among these, 2 compounds containing a remainder of glucamine exhibited moderate antiviral activity (compounds 9 and 15, EC50 = 5.42 µM, CC50 > 150 µM, SI50 > 28 and EC50 = 4.91 µM, CC50 > 150 µM, SI50 > 31, respectively). The difference between these compounds is that the first contains a phtalimide radical at position 4 and phosphoryl at position 5, whereas the latter contains a phenyl radical and a cyano group in the corresponding positions. However, they were considerably less active than the control drug, ganciclovir (EC50 = 0.32 µM, CC50 > 150 µM and SI50 > 476), in this assay. These and previously obtained data allow us to consider 1,3-oxazole as a promising backbone for the synthesis of new compounds with anti-HCMV activity.
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Acknowledgements
We would like to thank Enamine Ltd for the material and technical support. These studies were funded in whole or in part with Federal funds from the National Institute of Allergy and Infectious Diseases, National Institutes of Health, Department of Health and Human Services, under Contract Nos. HHSN272201100016I (MNP) and HHSN75N93019D00016 (SHJ).
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Abdurakhmanova, E.R., Brusnakov, M.Y., Golovchenko, O.V. et al. Synthesis and in vitro anticytomegalovirus activity of 5-hydroxyalkylamino-1,3-oxazoles derivatives. Med Chem Res 29, 1669–1675 (2020). https://doi.org/10.1007/s00044-020-02593-6
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DOI: https://doi.org/10.1007/s00044-020-02593-6