Abstract
The single enantiomers of two pyrimidine-based HIV-1 non-nucleoside reverse transcriptase inhibitors, 1 (MC1501) and 2 (MC2082), were tested in both cellular and enzyme assays. In general, the R forms were more potent than their S counterparts and racemates and (R)-2 was more efficient than (R)-1 and the reference compounds, with some exceptions. Interestingly, (R)-2 displayed a faster binding to K103N RT with respect to WT RT, while (R)-1 showed the opposite behavior. © 2012 American Chemical Society.
Original language | English |
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Pages (from-to) | 3558-3562 |
Journal | Journal of Medicinal Chemistry |
Volume | 55 |
Issue number | 7 |
DOIs | |
Publication status | Published - 12 Apr 2012 |