Fragment-Based Discovery of 6-Azaindazoles As Inhibitors of Bacterial DNA Ligase

[Image: see text] Herein we describe the application of fragment-based drug design to bacterial DNA ligase. X-ray crystallography was used to guide structure-based optimization of a fragment-screening hit to give novel, nanomolar, AMP-competitive inhibitors. The lead compound 13 showed antibacterial...

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Auteurs principaux: Howard, Steven, Amin, Nader, Benowitz, Andrew B., Chiarparin, Elisabetta, Cui, Haifeng, Deng, Xiaodong, Heightman, Tom D., Holmes, David J., Hopkins, Anna, Huang, Jianzhong, Jin, Qi, Kreatsoulas, Constantine, Martin, Agnes C. L., Massey, Frances, McCloskey, Lynn, Mortenson, Paul N., Pathuri, Puja, Tisi, Dominic, Williams, Pamela A.
Format: Artigo
Langue:Inglês
Publié: American Chemical Society 2013
Accès en ligne:https://ncbi.nlm.nih.gov/pmc/articles/PMC4027552/
https://ncbi.nlm.nih.gov/pubmed/24900632
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/ml4003277
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