Ciclopirox, an anti-fungal drug, has been shown to be effective in inhibiting the replication of Herpes Simplex Virus (HSV) -1 and -2. With a rise in the resistance of HSV strains to nucleotide analog treatments, the demand for the exploration of novel inhibitory compounds for the treatment of HSV infections has increased. In the present study, analogs of ciclopirox were synthesized to inhibit the activity of HSV. A number of these compounds displayed strong therapeutic potential with EC50values below that of acyclovir and minimal cytotoxicity. Structural comparison provides us with evidence of the importance of various structural motifs to the efficacy of ciclopirox and its derivatives, namely the hydrophobic groups at R4and R6of the core structure shown in the figure below. Together, these results represent an advance in the development of N-hydroxypyridones for the treatment of HSV.

Synthesis and evaluation of ciclopirox analogs as antiviral agents against herpes simplex virus 2

ACS Spring 2022

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