16566-20-4Relevant articles and documents
Quinoxalines useful as cytoprotective agents
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Page/Page column 34, (2020/08/16)
Provided herein are compounds of Formula I, pharmaceutical compositions thereof, and methods of their use for treating, preventing, or ameliorating one or more symptoms of a neurological disease, neurodegenerative disorder, or diabetes.
Synthetic method of quinoxaline-5-sulfonyl chloride
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, (2018/05/01)
The invention discloses a synthetic method of quinoxaline-5-sulfonyl chloride. The synthetic method is characterized by comprising the following steps that S1, a condensation reaction is carried out on 1,2-diamino-3-nitrobenzene with glyoxal for obtaining 5-nitroquinoxaline; S2, the 5-nitroquinoxaline reacts with a reducing agent for generating 5-aminoquinoxaline; and S3, diazotization reaction and Sandermeyer reaction are carried out on the 5-aminoquinoxaline for obtaining the quinoxaline-5-sulfonyl chloride. According to the process, a novel Sandermeyer reaction strategy is adopted for introducing sulfonyl chloride groups, the yield is greater than 70%, and the characteristics of novel process route, relatively mild reaction conditions and the like are achieved.
6,6-Fused heterocyclic ureas as highly potent TRPV1 antagonists
Sun, Wei,Kim, Hyo-Shin,Lee, Sunho,Jung, Aeran,Kim, Sung-Eun,Ann, Jihyae,Yoon, Suyoung,Choi, Sun,Lee, Jin Hee,Blumberg, Peter M.,Frank-Foltyn, Robert,Bahrenberg, Gregor,Schiene, Klaus,Stockhausen, Hannelore,Christoph, Thomas,Frormann, Sven,Lee, Jeewoo
, p. 803 - 806 (2015/02/19)
A series of N-[{2-(4-methylpiperidin-1-yl)-6-(trifluoromethyl)-pyridin-3-yl}methyl] N′-(6,6-fused heterocyclic) ureas have been investigated as hTRPV1 antagonists. Among them, compound 15 showed highly potent TRPV1 antagonism to capsaicin, with Ki(ant) = 0.2 nM, as well as antagonism to other activators, and it was efficacious in a pain model. A docking study of 15 with our hTRPV1 homology model indicates that there is crucial hydrogen bonding between the ring nitrogen and the receptor, contributing to its potency.