The design and synthesis of diaryl ether second generation HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTIs) with enhanced potency versus key clinical mutations.
Tucker TJ, Saggar S, Sisko JT, Tynebor RM, Williams TM, Felock PJ, Flynn JA, Lai MT, Liang Y, McGaughey GB, Liu M, Miller MD, Moyer G, Munshi V, Perlow-Poehnelt RA, Prasad S, Sanchez R, Torrent M, Vacca JP, Wan BL, Yan Y
Bioorganic & medicinal chemistry letters (2008), Volume 18, Page 2959
Abstract:
Using a combination of traditional Medicinal Chemistry/SAR analysis, crystallography, and molecular modeling, we have designed and synthesized a series of novel, highly potent NNRTIs that possess broad antiviral activity against a number of key clinical mutations.
Polymerases:
Topics:
Structure and Structure/Function, Reverse Transcriptase
Status:
| new | topics/pols set | partial results | complete | validated |
Results:
| Polymerase | Reference | Property | Result | Context |
|---|---|---|---|---|
| HIV RT | The design and synthesis of diaryl ether second generation HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTIs) with enhanced potency versus key clinical mutations. | Reverse Transcriptase Activity | Yes |