| Autor: |
Emtenas, H., Ahlin, K., Pinkner, J. S., Hultgren, S. J., Almqvist, F. |
| Zdroj: |
Journal of Combinatorial Chemistry; November 2002, Vol. 4 Issue: 6 p630-639, 10p |
| Abstrakt: |
A new method for the solid-phase synthesis of enantiomerically enriched highly substituted ring-fused 2-pyridinones 13 has been developed. The synthesis mediates introduction of substituents at two positions in the 2-pyridinone ring in a diverse manner and is suitable for parallel synthesis. 19F NMR spectroscopy was used as a tool to monitor each of the five steps in the reaction sequence. The optimized conditions thus obtained were then used to prepare a library of 20 2-pyridinones with high yields. The library members were chosen from a statistical multivariate design to ensure diversity and reliable data for structure−activity relationships. Screening of the library against the bacterial periplasmic chaperone PapD was performed using surface plasmon resonance. Three new 2-pyridinones with a higher affinity for the chaperone PapD than the previous best 13{10,1} were found, and important structural features could be deduced. |
| Databáze: |
Supplemental Index |
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