Structure-activity relationship study on anti-HIV 6-desfluoroquinolones.
On the basis of our recent findings that 6-aminoquinolones inhibit the HIV Tat-mediated transactivation, we have designed a broad series of derivatives identifying novel potent agents such as the 6-desfluoroquinolones 24 (HM12) and 27 (HM13), which showed pronounced anti-HIV activity in acutely, chronically, and latently HIV-1 infected cell cultures. We demonstrate here that highly potent molecules can be obtained by optimizing the substituent in the various positions of the quinolone nucleus.
Tabarrini
Oriana
O
Dipartimento di Chimica e Tecnologia del Farmaco, Università di Perugia, Via del Liceo 1, 06123 Perugia, Italy. oriana.tabarrini@unipg.it
Massari
Serena
S
Daelemans
Dirk
D
Stevens
Miguel
M
Manfroni
Giuseppe
G
Sabatini
Stefano
S
Balzarini
Jan
J
Cecchetti
Violetta
V
Pannecouque
Christophe
C
Fravolini
Arnaldo
A
D019380:Anti-HIV Agents / Q000737:chemistry* / Q000494:pharmacology; D002478:Cells, Cultured; D015658:HIV Infections / Q000188:drug therapy; D015497:HIV-1 / Q000187:drug effects; D006801:Humans; D011804:Quinolines / Q000737:chemistry / Q000494:pharmacology*; D015363:Quinolones; D013329:Structure-Activity Relationship
D019380:Anti-HIV Agents; C521529:HM-12 compound; D011804:Quinolines; D015363:Quinolones