|
|||||
|
|
Small molecule inhibitors of HIV RT Ribonuclease H |
|
| Authors: | Martin Di Grandi Matthew Olson Amar S Prashad Geraldine Bebernitz Amara Luckay Stanley Mullen Yongbo Hu Girija Krishnamurthy Keith Pitts John O’Connell |
| Institution: | Wyeth Research, 401 North Middletown Road, Pearl River, NY, United States |
| Abstract: | Two classes of compounds, thiocarbamates 1 and triazoles 2, have been identified as HIV RT RNase H inhibitors using a novel FRET-based HTS assay. The potent analogs in each series exhibited selectivity and were active in cell-based assays. In addition, saturable, 1:1 stoichiometric binding to target was established and time of addition studies were consistent with inhibition of RT-mediated HIV replication. |
| Keywords: | |
| 本文献已被 ScienceDirect 等数据库收录！ | |