Synthesis and biological evaluation of amidinourea derivatives against herpes simplex viruses

Anita Toscani, Rossana Denaro, Sergio Fernando Castillo Pacheco, Matteo Biolatti, Silvia Anselmi, Valentina Dell’oste, Daniele Castagnolo

Research output: Contribution to journalArticlepeer-review

7 Citations (Scopus)


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.

Original languageEnglish
Article number4927
Issue number16
Publication statusPublished - 2 Aug 2021


  • Amidines
  • Amidinourea
  • Antivirals
  • Guanidine
  • Herpes simplex virus


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