| Literature DB >> 18710207 |
Oriana Tabarrini1, 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.Entities:
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Year: 2008 PMID： 18710207 DOI： 10.1021/jm701585h
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446