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Synthesis and Biological Evaluation of Amidinourea Derivatives against Herpes Simplex Viruses.


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.

SUBMITTER: Toscani A 

PROVIDER: S-EPMC8398393 | biostudies-literature | 2021 Aug

REPOSITORIES: biostudies-literature

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Synthesis and Biological Evaluation of Amidinourea Derivatives against Herpes Simplex Viruses.

Toscani Anita A   Denaro Rossana R   Pacheco Sergio Fernando Castillo SFC   Biolatti Matteo M   Anselmi Silvia S   Dell'Oste Valentina V   Castagnolo Daniele D  

Molecules (Basel, Switzerland) 20210814 16


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, turnin  ...[more]

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