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