| Autor: |
Deibel, M. R., Jr., Bodnar, A. L., Yem, A. W., Wolfe, C. L., Heckaman, C. L., Bohanon, M. J., Mathews, W. R., Sweeney, M. T., Zurenko, G. E., Marotti, K. R., Boyle, T. P., Thorarensen, A. |
| Zdroj: |
Bioconjugate Chemistry; March 2004, Vol. 15 Issue: 2 p333-343, 11p |
| Abstrakt: |
Screening of our compound collection identified PNU-92560, a 2-[1,3,4]thiadiazolo[3,2-a]pyrimidine-6-carboxamide, as a novel antibacterial agent. Extensive analogue development identified that the 2-position of the thiadiazole could be functionalized with a linker that would allow the compound to be attached to a solid support. The extreme insolubility of the analogues prevented the mechanism of action for these compounds to be determined utilizing traditional methodology. The solid-supported compounds were utilized as affinity columns to identify elongation factor Tu (EF-Tu) as a putative target for this class of compounds. The activity of the compounds in a metabolic labeling experiments and in translation assay supports the identity of the target for these compounds to be EF-Tu. |
| Databáze: |
Supplemental Index |
| Externí odkaz: |
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