Patel, Meena V. published the artcileDiscovery of (R)-(3-fluoropyrrolidin-1-yl)(6-((5-(trifluoromethyl)pyridin-2-yl)oxy)quinolin-2-yl)methanone (ABBV-318) and analogs as small molecule Nav1.7/ Nav1.8 blockers for the treatment of pain, Quality Control of 623-50-7, the main research area is quinoline preparation sodium channel blocker SAR pharmacokinetic.
An effort to identify selective, CNS-penetrant Nav1.7 blockers with oral activity, improved selectivity, good drug-like properties, and safety led to the discovery of 2-substituted quinolines I [R = piperazine-1-carbonyl, cyclobutylcarbamoyl, 2-oxo-2-(1-piperidyl)ethoxy, etc.; R1 = 4-NCC6H4, 2-pyridyl, 5-(trifluoromethyl)-2-pyridyl, etc.] and quinolones II [R2 = 4-NCC6H4, 4-NCC6H4O; R3 = 1-piperidylmethyl, 1-piperidylmethyl] as potent small mol. Nav1.7 blockers. The design of these mols. focused on maintaining potency at Nav1.7, improving selectivity over the hERG channel, and overcoming phospholipidosis observed with the initial leads. The structure-activity relationship (SAR) studies leading to the discovery of compound I [R = (3R)-3-fluoropyrrolidine-1-carbonyl, R1 = 5-(trifluoromethyl)-2-pyridyl] were described herein. The compound I [R = (3R)-3-fluoropyrrolidine-1-carbonyl, R1 = 5-(trifluoromethyl)-2-pyridyl] displayed robust in vivo efficacy in both inflammatory and neuropathic rodent models of pain. The compound I [R = (3R)-3-fluoropyrrolidine-1-carbonyl, R1 = 5-(trifluoromethyl)-2-pyridyl] also inhibited Nav1.8, another sodium channel isoform that was an active target for the development of new pain treatments.
Bioorganic & Medicinal Chemistry published new progress about Amines Role: RCT (Reactant), RACT (Reactant or Reagent). 623-50-7 belongs to class esters-buliding-blocks, name is Ethyl 2-hydroxyacetate, and the molecular formula is C4H8O3, Quality Control of 623-50-7.
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