On June 26, 2014, Rooney, Lisa; Vidal, Agnes; D’Souza, Anne-Marie; Devereux, Nick; Masick, Brian; Boissel, Valerie; West, Ryan; Head, Victoria; Stringer, Rowan; Lao, Jianmin; Petrus, Matt J.; Patapoutian, Ardem; Nash, Mark; Stoakley, Natalie; Panesar, Moh; Verkuyl, J. Martin; Schumacher, Andrew M.; Petrassi, H. Michael; Tully, David C. published an article.Computed Properties of 152626-77-2 The title of the article was Discovery, Optimization, and Biological Evaluation of 5-(2-(Trifluoromethyl)phenyl)indazoles as a Novel Class of Transient Receptor Potential A1 (TRPA1) Antagonists. And the article contained the following:
A high throughput screening campaign identified 5-(2-chlorophenyl)indazole as an antagonist of the transient receptor potential A1 (TRPA1) ion channel with IC50 = 1.23 μM. Hit to lead medicinal chem. optimization established the SAR around the indazole ring system, demonstrating that a trifluoromethyl group at the 2-position of the Ph ring in combination with various substituents at the 6-position of the indazole ring greatly contributed to improvements in vitro activity. Further lead optimization resulted in the identification of compound I, a potent and selective antagonist of TRPA1 in vitro (IC50 = 0.015 μM), which has moderate oral bioavailability in rodents and demonstrates robust activity in vivo in several rodent models of inflammatory pain. The experimental process involved the reaction of 4-Bromo-5-methoxy-2-methylaniline(cas: 152626-77-2).Computed Properties of 152626-77-2
The Article related to fluoromethylphenyl indazole transient receptor potential a1 ion channel antagonist, trpa1 antagonist discovery optimization sar analgesic, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazoles and other aspects.Computed Properties of 152626-77-2
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