Novel Pyrazole-Containing Compounds Active against .

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ID: 64008
2019
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Abstract
In this study, a series of 49 five-membered heterocyclic compounds containing either a pyridine- or a pyrrole-type nitrogen were synthesized and tested against . Among them, only the 1,3,5-trisubstituted pyrazoles - exhibited minimum inhibitory concentration values in the low micromolar range, and some also exhibited an improved physicochemical profile without cytotoxic effects. Three pyrazoles were subjected to an animal tuberculosis efficacy model, and compound induced a statistically significant difference in lung bacterial counts compared with untreated mice. Moreover, to determine the target of this series, resistors were generated, and whole genome sequencing revealed mutations in the gene.
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poce2019novelacs Use this key to autocite in the manuscript while using SciMatic Manuscript Manager or Thesis Manager
Authors Poce, Giovanna;Consalvi, Sara;Venditti, Giulia;Alfonso, Salvatore;Desideri, Nicoletta;Fernandez-Menendez, Raquel;Bates, Robert H;Ballell, Lluis;Barros Aguirre, David;Rullas, Joaquin;De Logu, Alessandro;Gardner, Michelle;Ioerger, Thomas R;Rubin, Eric J;Biava, Mariangela;
Journal ACS medicinal chemistry letters
Year 2019
DOI
10.1021/acsmedchemlett.9b00204
URL
Keywords
molecular modeling drug development g protein-coupled receptors (gpcrs) ligand docking adrenergic receptors beta-adrenergic receptors computational drug design high throughput screening receptor structure

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