- Design, synthesis and biological evaluation of potent NAD+-dependent DNA ligase inhibitors as potential antibacterial agents. Part I: aminoalkoxypyrimidine carboxamides.
Design, synthesis and biological evaluation of potent NAD+-dependent DNA ligase inhibitors as potential antibacterial agents. Part I: aminoalkoxypyrimidine carboxamides.
Bioorganic & medicinal chemistry letters (2012-05-09)
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
PMID22560473
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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