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

  • Bioorg Med Chem. 2009 Jan 15;17(2):667-74. doi: 10.1016/j.bmc.2008.11.056.
Serena Massari  1 ,  Dirk Daelemans ,  Giuseppe Manfroni ,  Stefano Sabatini ,  Oriana Tabarrini ,  Christophe Pannecouque ,  Violetta Cecchetti
Affiliations
  • 1. Dipartimento di Chimica e Tecnologia del Farmaco, Università degli studi di Perugia, Via del Liceo 1, 06123 Perugia, Italy.
PMID: 19091580 DOI: 10.1016/j.bmc.2008.11.056
Abstract

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.