Title of article :
Design, synthesis, and biological evaluations of novel quinolones as HIV-1 non-nucleoside reverse transcriptase inhibitors
Author/Authors :
David Ellis، نويسنده , , Kelli L. Kuhen، نويسنده , , Beth Anaclerio، نويسنده , , Baogen Wu، نويسنده , , Karen Wolff، نويسنده , , Hong-Yin Chen، نويسنده , , Badry Bursulaya، نويسنده , , Jeremy Caldwell، نويسنده , , Donald Karanewsky، نويسنده , , Yun He، نويسنده ,
Abstract :
A novel series of quinolones was discovered as HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTIs) using a structure-based approach. The lead quinolones exhibited single digit nanomolar potency in the HIV-1 replication assays. The preliminary SAR of these quinolones was also established via systematic structural modifications. These novel and potent quinolones could serve as advanced leads for further optimization.
Keywords :
Quinolones , HIV-1 non-nucleoside reverse transcriptase inhibitor (NNRTI) , SAR , Molecule modeling , HIV replication
