Author/Authors :
Zachary K. Sweeney، نويسنده , , Sahaja Acharya، نويسنده , , Andrew Briggs، نويسنده , , James P. Dunn، نويسنده , , Todd R. Elworthy، نويسنده , , Jennifer Fretland، نويسنده , , Anthony M. Giannetti، نويسنده , , Gabrielle Heilek، نويسنده , , Yu Li، نويسنده , , Ann C. Kaiser، نويسنده , , Michael Martin، نويسنده , , Y. David Saito، نويسنده , , Mark Smith، نويسنده , , Judy M. Suh، نويسنده , , Steven Swallow، نويسنده , , Jeffrey Wu، نويسنده , , Julie Q. Hang، نويسنده , , Amy S. Zhou، نويسنده , , Klaus Klumpp، نويسنده ,
Abstract :
Novel non-nucleoside inhibitors of HIV-RT that contain pyridazinone isosteres were prepared, and a series of triazolinones were found to be potent inhibitors of HIV replication. These compounds were active against several NNRTI-resistant virus strains. Pharmacokinetic studies indicated that inhibitor 7e has good bioavailability in rats. Several fragments of inhibitor 7c were prepared, and the binding of these compounds to HIV-RT was analyzed by surface plasmon resonance spectroscopy.
Keywords :
Non-nucleoside , HIV-1 , reverse transcriptase , Human Immunodeficiency Virus
