Extended knowledge of 2081-44-9

If you¡¯re interested in learning more about 2081-44-9, below is a message from the blog Manager., 2081-44-9

Let¡¯s face it, organic chemistry can seem difficult to learn. Especially from a beginner¡¯s point of view. Like 2081-44-9, Name is Tetrahydro-2H-pyran-4-ol. In a document type is Article, introducing its new discovery., 2081-44-9

Thiazolopyridine ureas as novel antitubercular agents acting through inhibition of DNA gyrase B

A pharmacophore-based search led to the identification of thiazolopyridine ureas 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 homology model prompted exploration of the side chains at the thiazolopyridine ring C-5 position to access the ribose/solvent pocket. Potent compounds with GyrB IC 50 ? 1 nM and Mtb MIC ? 0.1 muM 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 physicochemical properties. Representative compounds were cocrystallized with Streptococcus pneumoniae (Spn) ParE; these confirmed the binding modes predicted by the homology 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.

If you¡¯re interested in learning more about 2081-44-9, below is a message from the blog Manager., 2081-44-9

Reference£º
Tetrahydropyran – Wikipedia,
Tetrahydropyran – an overview | ScienceDirect Topics