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.
Massari
Serena
S
Dipartimento di Chimica e Tecnologia del Farmaco, Università degli studi di Perugia, Via del Liceo 1, 06123 Perugia, Italy.
Daelemans
Dirk
D
Manfroni
Giuseppe
G
Sabatini
Stefano
S
Tabarrini
Oriana
O
Pannecouque
Christophe
C
Cecchetti
Violetta
V
D019380:Anti-HIV Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D006678:HIV / Q000187:drug effects; D006801:Humans; D015363:Quinolones / Q000138:chemical synthesis* / Q000494:pharmacology; D013329:Structure-Activity Relationship; D014158:Transcription, Genetic / Q000187:drug effects; D014779:Virus Replication / Q000187:drug effects
D019380:Anti-HIV Agents; D015363:Quinolones