| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1374060 | Bioorganic & Medicinal Chemistry Letters | 2012 | 6 Pages |
Abstract
A series of 2,6-disubstituted aminoalkoxypyrimidine carboxamides (AAPCs) with potent inhibition of bacterial NAD+-dependent DNA ligase was discovered through the use of structure-guided design. Two subsites in the NAD+-binding pocket were explored to modulate enzyme inhibitory potency: a hydrophobic selectivity region was explored through a series of 2-alkoxy substituents while the sugar (ribose) binding region of NAD+ was explored via 6-alkoxy substituents.
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Wenxin Gu, Tiansheng Wang, Francois Maltais, Brian Ledford, Joseph Kennedy, Yunyi Wei, Christian H. Gross, Jonathan Parsons, Leonard Duncan, S.J. Ryan Arends, Cameron Moody, Emanuele Perola, Jeremy Green, Paul S. Charifson,