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Aerojet, the No.Â .Novel classes of HIV-1 non-nucleoside inhibitors.
Continuous search for new anti-HIV-1 agents, including non-nucleoside inhibitors, has been ongoing. Three new classes of HIV-1 non-nucleoside inhibitors have been identified: a diarylsulfonylthiosemicarbazone [1], a bis(triazolyl) thiosemicarbazone [2] and a 2-hydroxypyridine-3-carboxaldehyde thiosemicarbazone [3]. The diarylsulfonylthiosemicarbazone [1] is a novel non-nucleoside inhibitor of HIV-1 reverse transcriptase that potently inhibits wild-type viral reverse transcriptase with an IC(50) of 0.73 nM, but exhibits only weak activity (IC(50) of 2.50 microM) against mutant HIV-1 reverse transcriptase enzymes that confer cross-resistance to AZT (or dideoxyinosine, ddI). The bis(triazolyl) thiosemicarbazone [2] is a novel thiosemicarbazone (EC(50) of 0.027 microM) and bis(triazolyl) piperazine (EC(50) of 0.18 microM) derivative that exhibits a potent non-nucleoside activity against the reverse transcriptase of HIV-1. The 2-hydroxypyridine-3-carboxaldehyde thiosemicarbazone [3] is a novel 1,4-dihydro-4-oxoquinoline-2-carboxaldehyde thiosemicarbazone (EC(50) of 0.043 microM) that potently inhibits the RT of wild-type HIV-1 and many mutant HIV-1 reverse transcriptase enzymes. In addition, 3, one of the potent compounds from the present series, exhibited antiviral activity in vivo against HIV-1 (including wild-type and AZT-selected mutants) in a mouse model, indicating the potential therapeutic utility of this compound.1. Field of the Invention
The present invention relates to the field of visual displays. More specifically, the present invention relates to an improved method and apparatus for light emitting diode (
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