Antiviral activity of amide-appended α-hydroxytropolones against herpes simplex virus-1 and -2.

ABSTRACT: α-Hydroxytropolones (αHTs) have potent antiviral activity against herpes simplex virus-1 and -2 (HSV-1 and HSV-2) in cell culture, including against acyclovir-resistant mutants, and as a result have the potential to be developed as antiviral drugs targeting these viruses. We recently described a convenient final-step amidation strategy to their synthesis, and this was used to generate 57 amide-substituted αHTs that were tested against hepatitis B virus. The following manuscript describes the evaluation of this library against HSV-1, as well as a subset against HSV-2. The structure-function analysis obtained from these studies demonstrates the importance of lipophilicity and rigidity to αHT-based anti-HSV potency, consistent with our prior work on smaller libraries. We used this information

SUBMITTER: Gazquez Casals A 

PROVIDER: S-EPMC10016935 | biostudies-literature | 2023 Mar

REPOSITORIES: biostudies-literature