1056879-33-4Relevant academic research and scientific papers
Structure-activity relationship study on anti-HIV 6-desfluoroquinolones
Tabarrini, Oriana,Massari, Serena,Daelemans, Dirk,Stevens, Miguel,Manfroni, Giuseppe,Sabatini, Stefano,Balzarini, Jan,Cecchetti, Violetta,Pannecouque, Christophe,Fravolini, Arnaldo
, p. 5454 - 5458 (2008)
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.
