Structure-activity relationship study on anti-HIV 6-desfluoroquinolones

Journal of Medicinal Chemistry
Oriana TabarriniArnaldo 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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Citations

Mar 24, 2011·Future Medicinal Chemistry·Oriana TabarriniVioletta Cecchetti
Nov 16, 2013·AIDS Research and Human Retroviruses·Caroline M RoyleAdriano Boasso
Sep 2, 2014·Malaria Journal·Richard M BeteckDavid D N'Da
Dec 3, 2014·European Journal of Medicinal Chemistry·Rangappa S KeriSrinivasa Budagumpi
Jul 6, 2010·Antiviral Research·Luis Miguel BedoyaPaulina Bermejo
Jun 9, 2016·Expert Opinion on Therapeutic Targets·Valentin Le DouceChristian Schwartz
Dec 26, 2008·Bioorganic & Medicinal Chemistry Letters·Giuseppe ManfroniArnaldo Fravolini
Jan 1, 2012·Biology·Guillaume Mousseau, Susana Valente
Sep 8, 2012·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Liming HuChengchu Zeng
Jul 6, 2019·Archiv der Pharmazie·Ruo WangWeixiong Shi
May 8, 2020·Future Medicinal Chemistry·Ishan WadiAbhinav Sinha
Dec 7, 2016·Acta Crystallographica. Section E, Crystallographic Communications·Hai Le Thi HongLuc Van Meervelt
Jul 25, 2020·The Journal of Pharmacy and Pharmacology·Yahya I AsiriMohd Z Hassan
Jul 17, 2020·Journal of Medicinal Chemistry·Tommaso FelicettiGiuseppe Manfroni
Oct 18, 2013·Journal of Medicinal Chemistry·Giuseppe ManfroniVioletta Cecchetti
Jun 7, 2014·Journal of Medicinal Chemistry·Manuela DonalisioOriana Tabarrini

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