33469-37-3Relevant academic research and scientific papers
Discovery of novel 2-aryl-4-bis-amide imidazoles (ABAI) as anti-inflammatory agents for the treatment of inflammatory bowel diseases (IBD)
Li, Ling,Yuan, Sijie,Lin, Lin,Yang, Fang,Liu, Ting,Xu, Chenglong,Zhao, Huiting,Chen, Jingxuan,Kuang, Peihua,Chen, Ting,Liao, Wenzhen,Chen, Jianjun
, (2022/01/28)
A series of 2-Aryl-4-Bis-amide Imidazoles (ABAI-1 to 30) were designed as anti-inflammatory agents. These compounds were synthesized and evaluated for the in vitro anti-inflammatory activities (inhibition of NO production and release of inflammatory cytok
BENZENESULFONAMIDE DERIVATIVES AS TRAP1 MODULATORS AND USES THEREOF
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Paragraph 00297; 00316; 00368-00369, (2021/09/26)
The present disclosure provides compounds of Formula (I): and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled compounds, and prodrugs thereof. The provided compounds may be tumor necrosis factor ("TNF") receptor associated protein 1 ("TRAP1") modulators (e.g., TRAP1 activators). The provided compounds may also rescue the activity in PTEN-induced kinase 1 ("PINK1") loss of function contexts. The provided compounds may also improve mitochondrial health, function, quality, quantity, and/or activity, and/or reduce the production of reactive oxygen species. The provided compounds may also refold or solubilize aggregated or misfolded proteins such as α-synuclein. The present disclosure also provides pharmaceutical compositions comprising the provided compounds; kits comprising the provided compounds or pharmaceutical compositions; and methods of using the provided compounds and pharmaceutical compositions (e.g., for treating a disease in a subject in need thereof).
Synthesis, structure, and neuroprotective properties of novel imidazolyl nitrones
Dhainaut, Alain,Tizot, André,Raimbaud, Eric,Lockhart, Brian,Lestage, Pierre,Goldstein, Solo
, p. 2165 - 2175 (2007/10/03)
A new series of imidazolyl nitrones spin traps has been synthesized and evaluated pharmacologically. The salient structural feature of these molecules is the presence of an imidazole moiety substituted by aromatic or heteroaromatic cycles. This connectivi
A convenient synthesis of perfluoroalkylated and fluorinated-aryl nitrogen bases by electrochemically induced SRN1 substitution
Medebielle, Maurice,Oturan, Mehmet Ali,Pinson, Jean,Saveant, Jean-Michel
, p. 1331 - 1339 (2007/10/03)
Indirect electrochemical reduction, by means of an aromatic anion mediator, of perfluoroalkyl halides (CF3Br, n-C4F9I, n-C6F13I, I(CF2)4I) in the presence of imidazole, 4(5)-nitroimidazole, 2-methyl-5-nitroimidazole, 2-(4′-methoxyphenyl)imidazole, imidazole-2-carboxaldehyde, 4(5)-nitroimidazole-2-carboxaldehyde, 5(6)-nitrobenzimidazole, purines (adenine, hypoxanthine, xanthine, theophylline, lumazine) and pyrimidine anions (uracil, cytosine, barbituric acid) yields the corresponding C-perfluoroalkylated nitrogen bases by an SRN1 mechanism. Aromatic nucleophilic substitution of some fluorinated aryl halides 1-iodo-2-(trifluoromethyl)benzene and 1-(4′-iodo-tetrafluorophenyl)-imidazole was also investigated and it was found that 1-iodo-2-(trifluoromethyl)benzene could react successfully under redox-catalyzed conditions with imidazole, 2-(4′-methoxyphenyl)imidazole anion, and uracil anion to give the corresponding 5-(fluorinated-aryl) nitrogen bases. In the case of 1-(4′-iodo-tetrafluorophenyl)imidazole, direct electrochemical radical nucleophilic substitution with 2-methyl-5-nitroimidazole and uracil was possible in DMSO. In this way new, 4-[2′,3′,5′,6′-tetrafluoro-4′-(imidazol-1″- yl)phenyl] nitrogen bases were obtained in good yields.
BETA-BLOCKING SUBSTITUTED IMIDAZOLES
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, (2008/06/13)
Novel substituted imidazoles and methods for their preparation are disclosed. These imidazoles, and their salts, exhibit pharmacological activity which includes antihypertensive activity and β-adrenergic blocking activity.
BETA-ADRENERGIC BLOCKING IMIDAZOLYLPHENOXY PROPANOLAMINES
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, (2008/06/13)
Substituted imidazoles and methods for their preparation are disclosed. These imidazoles, and their salts, exhibit pharmacological activity which includes antihypertensive activity and β-adrenergic blocking activity. STR1
CERTAIN ANTIHYPERTENSIVE 1-[2-[3-CARBAMOYL-4-HYDROXYPHENOXY]ALKYLENEAMINO]-HETEROCYCLIC PHENOXY-PROPANOL DERIVATIVES
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, (2008/06/13)
The invention relates to novel substituted phenyl ethers of the formula STR1 in which Ar represents a mono-or bi-cyclic carbocyclic aryl radical, or a mono-or bi-cyclic heterocyclic aryl radical bonded to a phenylene radical by way of a ring carbon atom,Ph represents a phenylene radical,n has the value 0 to 1 andalk represents alkylene having from 2 to 5 carbon atoms, the nitrogen atom and the oxygen atom or, if n is 0, the aromatic radical being separated from each other by at least two carbon atoms in the unbranched chain, andR 1 and R. sub.2 each represents, independently of the other, hydrogen or lower alkyl, or together represent lower alkylene, oxa-lower alkylene, thia-lower alkylene, aza-lower alkylene or N-lower alkyl-aza-lower alkylene, and salts thereof, especially pharmaceutically acceptable non-toxic acid addition salts. Such compounds possess, on the one hand, blocking properties towards β-adrenergic receptors and can therefore be used as β-receptor-blockers with or without cardioselectivity for the treatment of Angina pectoris, hypertrophic cardiomyopathy and heart rhythm disorders and also as blood-pressure-reducing agents. On the other hand, such compounds possess β-receptor-stimulating properties and can therefore be used as positively inotropically active agents, especially as cardiotonics, for the treatment of heart muscle insufficiency.
Trifluoromethylimidazoles and a method for their preparation
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, (2008/06/13)
4(5)-Trifluoromethylimidazoles having optional substituents in the 1 and 2 positions are provided. The novel 4(5)-trifluoromethylimidazoles are prepared by reacting a 1,1-dihalo-3,3,3-trifluoroacetone compound with an appropriate carboxaldehyde and ammoni
2-Pyrazinyl-trifluoromethylimidazoles and a method for their preparation
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, (2008/06/13)
4(5)-Trifluoromethylimidazoles having optional substituents in the 1 and 2 positions are provided. The novel 4(5)-trifluoromethylimidazoles are prepared by reacting a 1,1-dihalo-3,3,3-trifluoroacetone compound with an appropriate carboxaldehyde and ammoni
