Structure−Activity Relationship Study on Anti-HIV 6-Desfluoroquinolones
Journal of Medicinal Chemistry2008Vol. 51(17), pp. 5454–5458
Citations Over TimeTop 18% of 2008 papers
Oriana Tabarrini, Serena Massari, Dirk Daelemans, Miguel Stevens, Giuseppe Manfroni, Stefano Sabatini, Jan Balzarini, Violetta Cecchetti, Christophe Pannecouque, Arnaldo Fravolini
Abstract
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.
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