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2030-12-31
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- CDTS - Artigos de Periódicos [480]
- IOC - Artigos de Periódicos [12967]
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CHEMISTRY AND ANTI-HERPES SIMPLEX VIRUS TYPE 1 EVALUATION OF 4-SUBSTITUTED-1H-1,2,3-TRIAZOLE-NITROXYL-LINKED HYBRIDS
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Abstract
HSV disease is distributed worldwide. Anti-herpesvirus drugs are a problem in clinical settings, particularly in immunocompromised individuals undergoing herpes simplex virus type 1 infection. In this work, 4-substituted-1,2,3-1H-1,2,3-triazole linked nitroxyl radical derived from TEMPOL were synthesized, and their ability to inhibit the in vitro replication of HSV-1 was evaluated. The nitroxide derivatives were characterized by infrared spectroscopy and elemental analysis, and three of them had their crystal structures determined by single-crystal X-ray diffraction. Four hybrid molecules showed important anti-HSV-1 activity with IC<sub>50</sub> values ranged from 0.80 to 1.32 µM. In particular, one of the nitroxide derivatives was more active than Acyclovir (IC<sub>50</sub> = 0.99 µM). All compounds tested were more selective inhibitors than the reference antiviral drug. Among them, two compounds were 4.5 (IC<sub>50</sub> 0.80 µM; selectivity index CC<sub>50</sub>/IC<sub>50</sub> 3886) and 7.7 times (IC<sub>50</sub> 1.10 µM; selectivity index CC<sub>50</sub>/IC<sub>50</sub> 6698) more selective than acyclovir (IC<sub>50</sub> 0.99 µM; selectivity index CC<sub>50</sub>/IC<sub>50</sub>: 869). These nitroxide derivatives may be elected as leading compounds due to their antiherpetic activities and good selectivity.
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