Dengue is an important health issue in developing countries. Annually, Dengue Virus infects 390 million infections occur, leading to 500,000 hospitalizations and 20,000 deaths. Some N-allyl acridone derivatives have been studied as potential antivirals and have shown promising bioactivity. Docking studies suggested that they could interfere with viral IMPDH activity. We decide to prepare some isosters of these compounds to test their antibacterial and antiviral activities. In our group, we have developed an easy and direct method for the preparation of 2,3-diaminoquinolin-4(1H)-one, which was used to prepare compounds 1a-d and 2a-d as seen in Figure 1 in good yields. Docking studies were carried out in some dengue virus proteins (PDB codes: 1NF7, 5CUQ, 5HMY). Compound 2d had the lowest docking score in IMPDH, suggesting it could be an interesting lead for new antivirals. In other hand, their antibacterial properties were tested, compound 1b was active against Gram(+)bacteria.

Design and synthesis of N-substituted acridone derivatives as potential antibacterial and antiviral agents

253rd National Meeting (2017)

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