Qinghai Peng

TL;DR: PF-46396 represents the first small-molecule HIV-1 maturation inhibitor that is distinct in chemical class from betulinic acid-derived maturation inhibitors (e.g., DSB), demonstrating that molecules of diverse chemical classes can inhibit this mechanism.

TL;DR: Several 4-fluorobenzyl substituted azaindole hydroxamic acids showed potent antiviral activities in cell-based assays and offered a structurally simple scaffold for the development of novel HIV-1 IN inhibitors.

TL;DR: The design and synthesis of novel tricyclic N-hydroxy-dihydronaphthyridinones as potent, orally bioavailable HIV-1 integrase inhibitors displaying excellent ligand and lipophilic efficiencies are disclosed.

TL;DR: This study describes an HIV-1 dual reporter assay that allows for the simultaneous evaluation of the potential antiviral activities and cytotoxicities of compounds in a high throughput screen (HTS) format and shows that the antiviral and cytOToxic activities of compounds are reproducibly measured under screening conditions.

TL;DR: Polar groups at the β-position of the azaindole core are introduced thereby altering physical properties by lowering calculated log D values which resulted in attenuated clearance rates in human hepatocytes, suggesting opportunities to alter clearance parameters in future series.