88166-64-7Relevant articles and documents
A Series of Thiadiazolyl-Benzenesulfonamides Incorporating an Aromatic Tail as Isoform-Selective, Potent Carbonic Anhydrase II/XII Inhibitors
Banoglu, Erden,Bonardi, Alessandro,Gratteri, Paola,Supuran, Claudiu T.,Vullo, Daniela,Ercanl?, Taner,Gür Maz, Tu??e
, (2022/03/14)
We describe the synthesis of a series of thiadiazolyl-benzenesulfonamide derivatives carrying an aromatic tail linked by an amide linker (12–34), as human carbonic anhydrase (hCA) inhibitors. These thiadiazol derivatives were evaluated against four physiologically relevant CA isoforms (hCA I, II, IX, and XII), and demonstrated intriguing inhibitory activity against CA II with Ki values in the range of 2.4–31.6 nM. Besides hCA II, also hCA XII activity was potently inhibited by some of the derivatives (Ki=1.5–88.5 nM), producing dual inhibitors of both isoforms. Notably, compound 17 was the most potent dual CA II (Ki=3.1 nM) and XII (Ki=1.5 nM) inhibitor with a significant selectivity ratio over CA I and IX isoforms. In conclusion, although all compounds exhibited preferential activity towards hCA II, the nature of the substituents at the tail part of the main scaffold influenced the activity and selectivity toward other isoforms.
NOVEL NUCLEOSIDE OR NUCLEOTIDE DERIVATIVES, AND USES THEREOF
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Paragraph 0070; 0088, (2020/12/10)
The present disclosure relates to a novel nucleoside or nucleotide derivative, a racemate thereof, a stereoisomer thereof, or a pharmaceutically acceptable salt thereof; and a pharmaceutical composition for preventing or treating viral infection-associated diseases, containing the same as an active ingredient.
FUSED THIOPHENE DERIVATIVES AND THEIR USES
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Page/Page column 96, (2019/08/29)
The present invention relates to a new class of fused thiophene derivatives and their uses for treating diseases such as infection, cancer, metabolic diseases, cardiovascular diseases, iron storage disorders and inflammatory disorders.
Copper-Catalyzed Electrochemical C-H Amination of Arenes with Secondary Amines
Yang, Qi-Liang,Wang, Xiang-Yang,Lu, Jia-Yan,Zhang, Li-Pu,Fang, Ping,Mei, Tian-Sheng
supporting information, p. 11487 - 11494 (2018/09/13)
Electrochemical oxidation represents an environmentally friendly solution to conventional methods that require caustic stoichiometric chemical oxidants. However, C-H functionalizations merging transition-metal catalysis and electrochemical techniques are, to date, largely confined to the use of precious metals and divided cells. Herein, we report the first examples of copper-catalyzed electrochemical C-H aminations of arenes at room temperature using undivided electrochemical cells, thereby providing a practical solution for the construction of arylamines. The use of n-Bu4NI as a redox mediator is crucial for this transformation. On the basis of mechanistic studies including kinetic profiles, isotope effects, cyclic voltammetric analyses, and radical inhibition experiments, the reaction appears to proceed via a single-electron-transfer (SET) process, and a high valent Cu(III) species is likely involved. These findings provide a new avenue for transition-metal-catalyzed electrochemical C-H functionalization reactions using redox mediators.
BACE1 INHIBITORS
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Page/Page column 76, (2017/03/08)
The present invention provides a compound of formula I, having BACE1 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease.
Rh(III)-catalyzed cascade oxidative olefination/cyclization of picolinamides and alkenes via C-H activation
Cai, Shangjun,Chen, Chao,Shao, Peng,Xi, Chanjuan
supporting information, p. 3142 - 3145 (2014/06/23)
Rh(III)-catalyzed cascade oxidative alkenylation/cyclization of picolinamides and alkenes to furnish pyrido pyrrolone derivatives is described, in which three C-H bonds and one N-H bond broke, while one C-C bond and one C-N bond formed. The reaction proceeded with high yield and high regioselectivity and stereoselectivity. Moreover, copper acetate can also be used in catalytic amounts with O2 serving as the terminal oxidant.
8-benzamidochromen-4-one-2-carboxylic acids: Potent and selective agonists for the orphan G protein-coupled receptor GPR35
Funke, Mario,Thimm, Dominik,Schiedel, Anke C.,Müller, Christa E.
supporting information, p. 5182 - 5197 (2013/07/25)
8-Amido-chromen-4-one-2-carboxylic acid derivatives were identified as novel agonists at the G protein-coupled orphan receptor GPR35. They were characterized by a β-arrestin recruitment assay and optimized to obtain agonists with nanomolar potency for the
Certain aralkyloxy or aralkylthio-pyridyl-phthalimides and their use as herbicides
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, (2008/06/13)
N-substituted pyridyl tetrahydrophthalimides, intermediates therefor and synthesis thereof which are useful herbicides.
Certain aralkyloxy or thio-pyridyl-imidazo-pyridines and their herbicidal use
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, (2008/06/13)
3-Pyridyl-1,5-tetramethylenehydantoins, 4-pyridyl-1,2-tetramethylenetriazolidine-3,5-diones, and the thioanalogs thereof, which compounds are useful as herbicides.