Kale, Manoj G. published the artcileThiazolopyridine Ureas as Novel Antitubercular Agents Acting through Inhibition of DNA Gyrase B, Category: pyridine-derivatives, the publication is Journal of Medicinal Chemistry (2013), 56(21), 8834-8848, database is CAplus and MEDLINE.
A pharmacophore-based search led to the identification of thiazolopyridine ureas, e.g., I, as a novel scaffold with antitubercular activity acting through inhibition of DNA Gyrase B (GyrB) ATPase. Evaluation of the binding mode of thiazolopyridines in a Mycobacterium tuberculosis (Mtb) GyrB homol. model prompted exploration of the side chains at the thiazolopyridine ring C-5 position to access the ribose/solvent pocket. Potent compounds with GyrB IC50 â?1 nM and Mtb MIC â?0.1 μM were obtained with certain combinations of side chains at the C-5 position and heterocycles at the C-6 position of the thiazolopyridine core. Substitutions at C-5 also enabled optimization of the physicochem. properties. Representative compounds were cocrystd. with Streptococcus pneumoniae (Spn) ParE; these confirmed the binding modes predicted by the homol. model. The target link to GyrB was confirmed by genetic mapping of the mutations conferring resistance to thiazolopyridine ureas. The compounds are bactericidal in vitro and efficacious in vivo in an acute murine model of tuberculosis.
Journal of Medicinal Chemistry published new progress about 1351413-50-7. 1351413-50-7 belongs to pyridine-derivatives, auxiliary class Pyridine,Boronic acid and ester,Amide,Pyridine,Boronic Acids,Boronic acid and ester, name is (1-Methyl-2-oxo-1,2-dihydropyridin-4-yl)boronic acid, and the molecular formula is C6H8BNO3, Category: pyridine-derivatives.
Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem