Author/Authors :
Jeff A. O’Meara، نويسنده , , Araz Jakalian، نويسنده , , Steven Laplante، نويسنده , , Pierre R. Bonneau، نويسنده , , René Coulombe، نويسنده , , Anne-Marie Faucher، نويسنده , , Ingrid Guse، نويسنده , , Serge Landry، نويسنده , , Jennifer Racine، نويسنده , , Bruno Simoneau، نويسنده , , Bounkham Thavonekham، نويسنده , , Christiane Yoakim، نويسنده ,
Abstract :
High-throughput screening hit 1 was identified as a potent, broad-spectrum, non-nucleoside reverse transcriptase inhibitor (NNRTI) of HIV-1 replication. Analysis of the bound conformation of analogs of this inhibitor via molecular modeling and NMR contributed to the design of novel tertiary amide, carbamate, and thiocarbamate based NNRTIs.
Keywords :
Tertiary amide , Tertiary carbamate , Thio-tetrazole , NNRTI , Scaffold hopping , Tetrazole thioacetanilide