Abstract
Among many subtypes of influenza A viruses, influenza A(H1N1) and A(H3N2) subtypes are currently circulating among humans (WHO report 2014-15). Therapeutically, the emergence of viral resistance to currently available drugs (adamantanes and neuraminidase inhibitors) has heightened alarms for developing novel drugs that could address diverse targets in the viral replication cycle in order to improve treatment outcomes. To this regard, the design and synthesis of nucleoside analog inhibitors as potential anti-influenza A agents is a very active field of research nowadays. In this study, we designed and synthesized a series of hitherto unknown 6-methyl-7-substituted-7-deaza purine nucleoside analogs, and evaluated for their biological activities against influenza A virus strains, H1N1 and H3N2. From the viral inhibition assay, we identified some effective compounds, among which, compounds 5x (IC50 = 5.88 μM and 6.95 μM for H1N1 and H3N2, respectively) and 5z (IC50 = 3.95 μM and 3.61 μM for H1N1 and H3N2, respectively) demonstrated potent anti-influenza A activity. On the basis of selectivity index, we conceive that compound 5x may serve as a chemical probe of interest for further lead optimization studies with a general aim of dev...Continue Reading
References
Jan 8, 1993·Journal of Medicinal Chemistry·J V TuttleT A Krenitsky
Apr 16, 2004·Journal of Medicinal Chemistry·Anne B EldrupJie Xia
Sep 25, 2004·Antimicrobial Agents and Chemotherapy·David B OlsenSteven S Carroll
Oct 1, 2004·Journal of Medicinal Chemistry·Anne B EldrupDavid B Olsen
May 10, 2005·Journal of Ethnopharmacology·A KochD Soejarto
Jun 16, 2007·The Journal of Infectious Diseases·Varough M DeydeAlexander I Klimov
Aug 1, 2009·The Journal of Organic Chemistry·Peiyuan WangMichael J Sofia
Oct 23, 2010·Journal of Medicinal Chemistry·Runzhi WuBlake R Peterson
Dec 15, 2010·The Journal of Infectious Diseases·Tiffany G SheuLarisa V Gubareva
Feb 1, 1986·Journal of the American Chemical Society·V P Baillargeon, J K Stille
May 19, 2012·Bioorganic & Medicinal Chemistry Letters·Jiae KimKaren S Anderson
Jun 29, 2012·The Lancet Infectious Diseases·Fatimah S DawoodMarc-Alain Widdowson
Sep 13, 2012·PloS One·Nanyu HanYuguang Mu
Jan 30, 2013·Antimicrobial Agents and Chemotherapy·Andrés PizzornoGuy Boivin
Nov 26, 2013·Archiv der Pharmazie·Hanane ElayadiHassan B Lazrek
Nov 30, 2013·European Journal of Medicinal Chemistry·Sanmitra BarmanEric V Anslyn
Jan 9, 2014·Journal of Medicinal Chemistry·Petr NaušMichal Hocek
Feb 22, 2014·PloS One·Goran OrozovicBjörn Olsen
Apr 29, 2014·Vaccine·UNKNOWN WHO
Jun 24, 2014·Chemical Biology & Drug Design·Jingjing GaoDingjue Ji
Jul 22, 2014·Journal of Medical Virology·Vanessa CorreiaHelena Rebelo-de-Andrade
Jan 23, 2015·TheScientificWorldJournal·Dalya Al-SaadPaolo Quadrelli
Apr 17, 2015·Chemistry & Biodiversity·Shu-Ting ChungAn-Rong Lee
Aug 28, 2015·European Journal of Medicinal Chemistry·Meng-I LinChung-Ming Sun
Citations
Oct 21, 2016·Medicinal Research Reviews·Annelies Stevaert, Lieve Naesens
Oct 27, 2018·Journal of Enzyme Inhibition and Medicinal Chemistry·M Lourdes SciúE Laura Moyano
Aug 24, 2017·Medicinal Research Reviews·Pavla Perlíková, Michal Hocek
Sep 16, 2020·Molecular Diversity·Olga V AndreevaVladimir E Kataev
Feb 8, 2021·European Journal of Medicinal Chemistry·Xia LinWeisen Lan
Apr 16, 2021·ChemMedChem·Cai LinSerge Van Calenbergh
Jun 23, 2021·Bioorganic Chemistry·Arif MermerYakup Sirin
Aug 11, 2021·International Journal for Parasitology. Drugs and Drug Resistance·Cai LinSerge Van Calenbergh
Apr 3, 2018·Chemical Reviews·Yi ZhuF Dean Toste