McKerrall, Steven J. published the artcileStructure- and Ligand-Based Discovery of Chromane Arylsulfonamide Nav1.7 Inhibitors for the Treatment of Chronic Pain, Quality Control of 343338-28-3, the main research area is pain analgesic chromane arylsulfonamide sodium channel crystal structure pharmacokinetics.
Using structure- and ligand-based design principles, a novel series of piperidyl chromane arylsulfonamide Nav1.7 inhibitors was discovered. Early optimization focused on improvement of potency through refinement of the low energy ligand conformation and mitigation of high in vivo clearance. An in vitro hepatotoxicity hazard was identified and resolved through optimization of lipophilicity and LLE to arrive at GNE-616 (24(I)), a highly potent, metabolically stable, subtype selective inhibitor of Nav1.7. I showed a robust PK/PD response in a Nav1.7 dependent mouse model and site-directed mutagenesis was used to identify residues critical for the isoform selectivity profile of I.
Journal of Medicinal Chemistry published new progress about Analgesics. 343338-28-3 belongs to class amides-buliding-blocks, name is (S)-2-Methylpropane-2-sulfinamide, and the molecular formula is C4H11NOS, Quality Control of 343338-28-3.
Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics