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Triazines

  • Regioisomerization of Antimalarial Drug WR99210 Explains the Inactivity of a Commercial Stock
    Chemistry; Biosynthesis
    Regioisomerization of Antimalarial Drug WR99210 Explains the Inactivity of a Commercial Stock

    WR99210, a former antimalarial drug candidate now widely used for the selection of Plasmodium transfectants, selectively targets the parasite’s dihydrofolate reductase thymidine synthase bifunctional enzyme (DHFR-TS) but not human DHFR, which is not fused with TS. Accordingly, WR99210 and plasmids expressing the human dhfr gene have become valued tools for the genetic modification of parasites in the laboratory....

    T. Parks Remcho, Sravanthi D. Guggilapu, Phillip Cruz, Glenn A. Nardone, Gavin Heffernan, Robert D. O’Connor, Carole A. Bewley, Thomas E. Wellems, Kristin D. Lane
  • Antiviral Agents
    ADS-J1 Inhibits HIV-1 Entry by Interacting with gp120 and Does Not Block Fusion-Active gp41 Core Formation
    Emmanuel González-Ortega, Maria-Pau Mena, Marc Permanyer, Ester Ballana, Bonaventura Clotet, José A. Esté
  • Pharmacology
    Antiviral Properties, Metabolism, and Pharmacokinetics of a Novel Azolo-1,2,4-Triazine-Derived Inhibitor of Influenza A and B Virus Replication
    Inna Karpenko, Sergey Deev, Oleg Kiselev, Valerey Charushin, Vladimir Rusinov, Eugeney Ulomsky, Ella Deeva, Dmitry Yanvarev, Alexander Ivanov, Olga Smirnova, Sergey Kochetkov, Oleg Chupakhin, Marina Kukhanova
  • Antiviral Agents
    ADS-J1 Inhibits Human Immunodeficiency Virus Type 1 Entry by Interacting with the gp41 Pocket Region and Blocking Fusion-Active gp41 Core Formation
    Hongtao Wang, Zhi Qi, Angi Guo, Qinchao Mao, Hong Lu, Xiuli An, Chenglai Xia, Xiaojuan Li, Asim K. Debnath, Shuguang Wu, Shuwen Liu, Shibo Jiang
  • Experimental Therapeutics
    Triazine Inhibits Toxoplasma gondii Tachyzoites In Vitro and In Vivo
    Ernest J. Mui, David Jacobus, Wilbur K. Milhous, Guy Schiehser, Honghue Hsu, Craig W. Roberts, Michael J. Kirisits, Rima McLeod
  • Antiviral Agents
    A Series of Diaryltriazines and Diarylpyrimidines Are Highly Potent Nonnucleoside Reverse Transcriptase Inhibitors with Possible Applications as Microbicides
    Yven Van Herrewege, Guido Vanham, Jo Michiels, Katrien Fransen, Luc Kestens, Koen Andries, Paul Janssen, Paul Lewi
  • Experimental Therapeutics
    Trypanocidal Activity of Melamine-Based Nitroheterocycles
    Mhairi L. Stewart, Gorka Jimenez Bueno, Alessandro Baliani, Burkhard Klenke, Reto Brun, Janice M. Brock, Ian H. Gilbert, Michael P. Barrett
  • Mechanisms of Action: Physiological Effects
    Novel Saccharomyces cerevisiae Screen Identifies WR99210 Analogues That Inhibit Mycobacterium tuberculosis Dihydrofolate Reductase
    A'Lissa B. Gerum, Jonathan E. Ulmer, David P. Jacobus, Norman P. Jensen, David R. Sherman, Carol Hopkins Sibley
  • Antiviral Agents
    RFI-641, a Potent Respiratory Syncytial Virus Inhibitor
    Clayton C. Huntley, William J. Weiss, Anna Gazumyan, Aron Buklan, Boris Feld, William Hu, Thomas R. Jones, Timothy Murphy, Antonia A. Nikitenko, Bryan O'Hara, Gregory Prince, Susan Quartuccio, Yuri E. Raifeld, Philip Wyde, John F. O'Connell
  • Experimental Therapeutics
    In Vitro and In Vivo Activities of Trybizine Hydrochloride against Various Pathogenic Trypanosome Species
    Ronald Kaminsky, Reto Brun

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