Current therapy against herpes simplex viruses (HSV) relies on the use of a few nucleoside antivirals such as acyclovir, famciclovir and valacyclovir. However, the current drugs are ineffective against latent and drug-resistant HSV infections. A series of amidinourea compounds, designed as analogues of the antiviral drug moroxydine, has been synthesized and evaluated as potential non-nucleoside anti-HSV agents. Three compounds showed micromolar activity against HSV-1 and low cytotoxicity, turning to be promising candidates for future optimization. Preliminary mode of action studies revealed that the new compounds act in an early stage of the HSV replication cycle, just after the viral attachment and the entry phase of the infection.

Synthesis and Biological Evaluation of Amidinourea Derivatives against Herpes Simplex Viruses [*Valentina Dell'Oste, Daniele Castagnolo: co-corresponding authors]

Sergio Fernando Castillo Pacheco;Matteo Biolatti;Valentina Dell’Oste
Co-last
;
2021

Abstract

Current therapy against herpes simplex viruses (HSV) relies on the use of a few nucleoside antivirals such as acyclovir, famciclovir and valacyclovir. However, the current drugs are ineffective against latent and drug-resistant HSV infections. A series of amidinourea compounds, designed as analogues of the antiviral drug moroxydine, has been synthesized and evaluated as potential non-nucleoside anti-HSV agents. Three compounds showed micromolar activity against HSV-1 and low cytotoxicity, turning to be promising candidates for future optimization. Preliminary mode of action studies revealed that the new compounds act in an early stage of the HSV replication cycle, just after the viral attachment and the entry phase of the infection.
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amidinourea; herpes simplex virus; guanidine; antivirals; amidines
Anita Toscani, Rossana Denaro, Sergio Fernando Castillo Pacheco , Matteo Biolatti , Silvia Anselmi , Valentina Dell’Oste, Daniele Castagnolo
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Utilizza questo identificativo per citare o creare un link a questo documento: http://hdl.handle.net/2318/1796930
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