Sutherland, Hamish S.’s team published research in Journal of Medicinal Chemistry in 53 | CAS: 870459-90-8

Journal of Medicinal Chemistry published new progress about 870459-90-8. 870459-90-8 belongs to pyridine-derivatives, auxiliary class Trifluoromethyl,Pyridine,Fluoride,Boronic acid and ester,Boronic Acids,Boronic acid and ester, name is (4-(Trifluoromethyl)pyridin-2-yl)boronic acid, and the molecular formula is C4HN5, HPLC of Formula: 870459-90-8.

Sutherland, Hamish S. published the artcileSynthesis and Structure-activity Relationships of Antitubercular 2-Nitroimidazooxazines Bearing Heterocyclic Side Chains, HPLC of Formula: 870459-90-8, the publication is Journal of Medicinal Chemistry (2010), 53(2), 855-866, database is CAplus and MEDLINE.

Previously, biphenyl analogs of the antituberculosis drug PA-824 were found to display improved potencies against M. tuberculosis but were poorly soluble Heterobiaryl analogs of these, e.g., I (X = 2,5-thiophenediyl, R = 4-F), in which the first Ph ring was replaced with various 5-membered ring heterocycles, were prepared with the aim of identifying potent new candidates with improved aqueous solubility The compounds were constructed by coupling the chiral 2-nitroimidazooxazine II with various halomethyl-substituted arylheterocycles, by cycloadditions to a propargyl ether derivative of this alc., or by Suzuki couplings on haloheterocyclic Me ether derivatives The arylheterocyclic compounds were all more hydrophilic than their corresponding biphenyl analogs, and several showed solubility improvements. 1-Methylpyrazole, e.g., I (X = 1-methyl-3,5-pyrazolediyl, R = 4-F3C), 1,3-linked-pyrazole, e.g., I (X = 1,3-pyrazolediyl, R = 4-F), 2,4-linked-triazole, e.g., I [X = 1,2,3-triazole-2,4-diyl, R = 4-(CF3O)] and tetrazole analogs, e.g., I (X = 2,5-tetrazolediyl, R = H) had 3- to 7-fold higher MIC potencies against replicating M. tuberculosis than predicted by their lipophilicities. Two pyrazole analogs were >10-fold more efficacious than the parent drug in a mouse model of acute M. tuberculosis infection, and one displayed a 2-fold higher solubility

Journal of Medicinal Chemistry published new progress about 870459-90-8. 870459-90-8 belongs to pyridine-derivatives, auxiliary class Trifluoromethyl,Pyridine,Fluoride,Boronic acid and ester,Boronic Acids,Boronic acid and ester, name is (4-(Trifluoromethyl)pyridin-2-yl)boronic acid, and the molecular formula is C4HN5, HPLC of Formula: 870459-90-8.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem