Design, synthesis and biological evaluation of potent NAD+-dependent DNA ligase inhibitors as potential antibacterial agents. Part I: aminoalkoxypyrimidine carboxamides

Bioorganic & Medicinal Chemistry Letters
Wenxin GuPaul S Charifson

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.

References

Jul 18, 2003·The Journal of Biological Chemistry·Heike Brötz-OesterheltHarald Labischinski
Dec 20, 2005·Nucleic Acids Research·Sandeep Kumar SrivastavaRavishankar Ramachandran

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Citations

May 14, 2014·Analytical and Bioanalytical Chemistry·Eva StejskalováMiroslav Fojta
May 15, 2015·Organic & Biomolecular Chemistry·Giulia PergolizziGerd K Wagner
Jan 21, 2017·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Malgorzata Korycka-MachalaJaroslaw Dziadek
Dec 1, 2017·Frontiers in Molecular Biosciences·Michael A ReicheValerie Mizrahi
Nov 8, 2017·Current Medicinal Chemistry·Lanhua Yi, Xin Lü
Feb 23, 2017·Proceedings of the National Academy of Sciences of the United States of America·Mihaela-Carmen UnciuleacStewart Shuman
Sep 2, 2016·Bioscience Reports·Giulia PergolizziRichard Peter Bowater
Jul 3, 2018·ACS Infectious Diseases·Ramkumar IyerAlice L Erwin

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