Antiretroviral (HIV-1) activity of azulene derivatives

  • Bioorg Med Chem. 2016 Apr 15;24(8):1653-7. doi: 10.1016/j.bmc.2016.02.038.
Julia Peet  1 ,  Anastasia Selyutina  1 ,  Aleksei Bredihhin  2
Affiliations
  • 1. Institute of Technology, University of Tartu, Nooruse 1, 50411 Tartu, Estonia.
  • 2. Institute of Technology, University of Tartu, Nooruse 1, 50411 Tartu, Estonia. Electronic address: [email protected].
PMID: 26964674 DOI: 10.1016/j.bmc.2016.02.038
Abstract

The antiretroviral activity of azulene derivatives was detected for the first time. A series of eighteen diversely substituted azulenes was synthesized and tested in vitro using HIV-1 based virus-like particles (VLPs) and infectious HIV-1 virus in U2OS and TZM-bl cell lines. Among the compounds tested, the 2-hydroxyazulenes demonstrated the most significant activity by inhibiting HIV-1 replication with IC50 of 2-10 and 8-20 μM for the VLPs and the infectious virus, respectively. These results indicate that azulene derivatives may be potentially useful candidates for the development of antiretroviral agents.

Keywords
Antiviral; Azulene; HIV; HIV-1 inhibition.
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