Category: 870459-90-8

Arhancet, Graciela B. published the artcileDiscovery and SAR of PF-4693627, a potent, selective and orally bioavailable mPGES-1 inhibitor for the potential treatment of inflammation, Recommanded Product: (4-(Trifluoromethyl)pyridin-2-yl)boronic acid, the publication is Bioorganic & Medicinal Chemistry Letters (2013), 23(4), 1114-1119, database is CAplus and MEDLINE.

Inhibition of mPGES-1, the terminal enzyme in the arachidonic acid/COX pathway to regulate the production of pro-inflammatory prostaglandin PGE2, is considered an attractive new therapeutic target for safe and effective anti-inflammatory drugs. The discovery of a novel series of orally active, selective benzoxazole piperidinecarboxamides as mPGES-1 inhibitors is described. Structure-activity optimization of lead compound with cyclohexyl carbinols resulted in a compound, which showed excellent in vitro potency and selectivity against COX-2, and reasonable pharmacokinetic properties. Further SAR studies of the benzoxazole ring substituents lead to a novel series of highly potent compounds with improved PK profile, which were effective in a carrageenan-stimulated guinea pig air pouch model of inflammation. Based on its excellent in vitro and in vivo pharmacol., pharmacokinetic and safety profile and ease of synthesis, PF-4693627 (I) was advanced to clin. studies.

Bioorganic & Medicinal Chemistry Letters 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 C6H5BF3NO2, Recommanded Product: (4-(Trifluoromethyl)pyridin-2-yl)boronic acid.

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

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

Dropinski, James F. published the artcileSynthesis and biological activities of novel arylindole-2-carboxylic acid analogs as PPARγ partial agonists, Name: (4-(Trifluoromethyl)pyridin-2-yl)boronic acid, the publication is Bioorganic & Medicinal Chemistry Letters (2005), 15(22), 5035-5038, database is CAplus and MEDLINE.

A series of novel arylindole-2-carboxylic acids has been identified as potent selective PPARγ modulators. Their chem. synthesis and in vitro activities are discussed. The indole I was selected for in vivo testing in the db/db mouse model of type 2 diabetes and resulted in reduction of hyperglycemia at comparable plasma exposure when compared to rosiglitazone.

Bioorganic & Medicinal Chemistry Letters 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 C6H5BF3NO2, Name: (4-(Trifluoromethyl)pyridin-2-yl)boronic acid.

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