Roecker, Anthony J. published the artcileDiscovery of selective, orally bioavailable, N-linked arylsulfonamide Nav1.7 inhibitors with pain efficacy in mice, Synthetic Route of 942603-91-0, the publication is Bioorganic & Medicinal Chemistry Letters (2017), 27(10), 2087-2093, database is CAplus and MEDLINE.
The voltage-gated sodium channel Nav1.7 is a genetically validated target for the treatment of pain with gain-of-function mutations in man eliciting a variety of painful disorders and loss-of-function mutations affording insensitivity to pain. Unfortunately, drugs thought to garner efficacy via Nav1 inhibition have undesirable side effect profiles due to their lack of selectivity over channel isoforms. Herein we report the discovery of a novel series of orally bioavailable arylsulfonamide Nav1.7 inhibitors with high levels of selectivity over Nav1.5, the Nav isoform responsible for cardiovascular side effects, through judicious use of parallel medicinal chem. and physicochem. property optimization. This effort produced inhibitors such as compound 5 with excellent potency, selectivity, behavioral efficacy in a rodent pain model, and efficacy in a mouse itch model suggestive of target modulation.
Bioorganic & Medicinal Chemistry Letters published new progress about 942603-91-0. 942603-91-0 belongs to esters-buliding-blocks, auxiliary class Other Aliphatic Fused-Heterocycles, name is Ethyl 2-methylene-5-oxohexahydro-1H-pyrrolizine-7a-carboxylate, and the molecular formula is C11H15NO3, Synthetic Route of 942603-91-0.
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