Studies on anti-HIV quinolones: New insights on the C-6 position

The 6-desfluoroquinolones which have been developed by our group represent a promising class of compounds for the treatment of HIV infection since they act on transcriptional regulation, a crucial step in the replication cycle that has not been clinically exploited, yet. Focussing attention on the N-1 and C-6 positions, a novel series of quinolones has been synthesized. New SAR insights have been obtained, in particular, the hydroxyl group emerged as a suitable C-6 substituent when coupled with the appropriate arylpiperazine at the neighboring C-7 position.

Groups with different chemical–physical properties have been explored to further investigate the role of the C-6 substituent in the anti-HIV activity/cytotoxicity of the quinolone derivatives.Figure optionsDownload as PowerPoint slide