Application In Synthesis of 4-Chloro-2-fluoropyridine. The protonation of heteroatoms in aromatic heterocycles can be divided into two categories: lone pairs of electrons are in the aromatic ring conjugated system; and lone pairs of electrons do not participate. Compound: 4-Chloro-2-fluoropyridine, is researched, Molecular C5H3ClFN, CAS is 34941-92-9, about Tetrahydrofuran-Based Transient Receptor Potential Ankyrin 1 (TRPA1) Antagonists: Ligand-Based Discovery, Activity in a Rodent Asthma Model, and Mechanism-of-Action via Cryogenic Electron Microscopy. Author is Terrett, Jack A.; Chen, Huifen; Shore, Daniel G.; Villemure, Elisia; Larouche-Gauthier, Robin; Dery, Martin; Beaumier, Francis; Constantineau-Forget, Lea; Grand-Maitre, Chantal; Lepissier, Luce; Ciblat, Stephane; Sturino, Claudio; Chen, Yong; Hu, Baihua; Lu, Aijun; Wang, Yunli; Cridland, Andrew P.; Ward, Stuart I.; Hackos, David H.; Reese, Rebecca M.; Shields, Shannon D.; Chen, Jun; Balestrini, Alessia; Riol-Blanco, Lorena; Lee, Wyne P.; Liu, John; Suto, Eric; Wu, Xiumin; Zhang, Juan; Ly, Justin Q.; La, Hank; Johnson, Kevin; Baumgardner, Matt; Chou, Kang-Jye; Rohou, Alexis; Rouge, Lionel; Safina, Brian S.; Magnuson, Steven; Volgraf, Matthew.
Transient receptor potential ankyrin 1 (TRPA1) is a nonselective calcium-permeable ion channel highly expressed in the primary sensory neurons functioning as a polymodal sensor for exogenous and endogenous stimuli and has generated widespread interest as a target for inhibition due to its implication in neuropathic pain and respiratory disease. Herein, we describe the optimization of a series of potent, selective, and orally bioavailable TRPA1 small mol. antagonists, leading to the discovery of a novel tetrahydrofuran-based linker. Given the balance of physicochem. properties and strong in vivo target engagement in a rat AITC-induced pain assay, compound (I) was progressed into a guinea pig ovalbumin asthma model where it exhibited significant dose-dependent reduction of inflammatory response. Furthermore, the structure of the TRPA1 channel bound to compound (II) was determined via cryogenic electron microscopy to a resolution of 3 Å, revealing the binding site and mechanism of action for this class of antagonists. Tetrahydrofurans
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