Abstract
Click and go: By using click chemistry based on a new triazole forming reaction condition (see scheme), over 100 triazole compounds generated in microtiter plates from a core structure were screened for HIV protease inhibition in situ without product isolation. Potent inhibitors, active at nanomolar concentrations, against the wild type and drug resistant mutants were identified.
| Original language | English |
|---|---|
| Pages (from-to) | 1246-1248 |
| Number of pages | 3 |
| Journal | ChemBioChem |
| Volume | 4 |
| Issue number | 11 |
| DOIs | |
| Publication status | Published - 7 Nov 2003 |
| Externally published | Yes |
Keywords
- Click chemistry
- Enzyme
- HIV protease
- Inhibitors
- Screening
ASJC Scopus subject areas
- Drug Discovery
- Organic Chemistry
- Biochemistry, Genetics and Molecular Biology(all)
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Cite this
Brik, A., Muldoon, J., Lin, Y. C., Elder, J. H., Goodsell, D. S., Olson, A. J., Fokin, V. V., Sharpless, K. B., & Wong, C. H. (2003). Rapid Diversity-Oriented Synthesis in Microtiter Plates for in Situ Screening of HIV Protease Inhibitors. ChemBioChem, 4(11), 1246-1248. https://doi.org/10.1002/cbic.200300724