56857-02-4Relevant academic research and scientific papers
HISTONE ACETYLTRANSFERASE (HAT) INHIBITOR AND USE THEREOF
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Paragraph 0614-0615, (2021/02/25)
The present invention relates to a histone acetyltransferase (HAT) inhibitor. Provided are a compound represented by general formula I, a pharmaceutically acceptable salt, a stereoisomer, an enantiomer, a diastereomer, an atropisomer, a racemate, a polymorph, a solvate or an isotope-labeled compound (including deuterium substitution) thereof, a preparation method therefor, a pharmaceutical composition comprising the same, and use thereof in the treatment of various HAT-related diseases or conditions.
Efficient synthesis of dibenzazepine lactams via a sequential Pd-catalyzed amination and aldol condensation reaction
Song, Ha-Jeong,Yoon, Eunyoung,Heo, Jung-Nyoung
supporting information, (2019/12/27)
A simple and efficient reaction was developed for the synthesis of dibenzazepine lactam derivatives. The core 7-membered azepine ring was formed by a stepwise sequence involving a palladium-catalyzed amination and an aldol condensation.
Synthesis of 4-thiophen-2′-yl-1,4-dihydropyridines as potentiators of the CFTR chloride channel
Cateni, Francesca,Zacchigna, Marina,Pedemonte, Nicoletta,Galietta, Luis J.V.,Mazzei, Marco T.,Fossa, Paola,Giampieri, Michele,Mazzei, Mauro
experimental part, p. 7894 - 7903 (2010/04/05)
The gating of the CFTR chloride channel is altered by a group of mutations that cause cystic fibrosis. This gating defect may be corrected by small molecules called potentiators. Some 1,4-dihydropyridine (DHP) derivatives, bearing a thiophen-2-yl and a furanyl ring at the 4-position of the nucleus, were prepared and tested as CFTR potentiators. In particular, we evaluated the ability of novel DHPs to enhance the activity of the rescued ΔF508-CFTR as measured with a functional assay based on the halide-sensitive yellow fluorescent protein. Most DHPs showed an effect comparable to or better than that of the reference compound genistein. The potency was instead significantly improved, with some compounds, such as 3g, 3h, 3n, 4a, 4b, and 4d, having a half effective concentration in the submicromolar range. CoMFA analysis gave helpful suggestions to improve the activity of DHPs.
The effects of pendant vs. fused thiophene attachment upon the luminescence lifetimes and electrochemistry of tris(2,2′-bipyridine)ruthenium(II) complexes
Nurkkala, Lasse J.,Steen, Robert O.,Friberg, Henrik K. J.,Haeggstroem, Johanna A.,Bernhardt, Paul V.,Riley, Mark J.,Dunne, Simon J.
scheme or table, p. 4101 - 4110 (2009/02/07)
The electrochemical and photophysical properties for a range of tris(2,2′-bipyridine)ruthenium(II) complexes in which a thiophene substituent is attached to one of the bipyridine ligands by either a pendant or a fused mode have been determined. The fused mode of attachment eliminates torsional movement between the thiophene unit and the chelating bipyridine, thereby offering optimal overlap between the ?-systems of the chelating unit and the attached thiophene unit. The electrochemical properties of these complexes were found to be similar; however, the luminescence lifetimes and intensities (in CH3CN at room temperature) were found to be correlated to the mode of attachment. The longest luminescence lifetime was observed for the complex [Ru(bpy)2{4-(thiophen-2-yl)-2,2′-bipyridine}] 2+ (3000 ns), as compared to the prototypic [Ru(bpy) 3]2+ (1745 ns). This complex also had the highest quantum yield (0.045). In the four isomeric complexes, where the thiophene ring was fused to the b or c face of the pyridine ring, the lifetimes fell in the interval 275-1510 ns, and the quantum yield ranged between 0.0047 and 0.014. Wiley-VCH Verlag GmbH & Co. KGaA, 2008.
Oxaboroles and salts thereof, and their use as biocides
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, (2008/06/13)
A method for the protection of a medium by susceptible to microbial attack by the treatment of the medium with an oxaborale or a salt of an oxaborale.
New isomeric classes of topically active ocular hypotensive carbonic anhydrase inhibitors: 5-Substituted thieno[2,3-b]thiophene-2-sulfonamides and 5-substituted theio[3,2-b]thiophene-2-sulfonamides
Prugh,Hartman,Mallorga,McKeever,Michelson,Murcko,Schwam,Smith,Sondey,Springer,Sugrue
, p. 1805 - 1818 (2007/10/02)
A series of 5-substituted thieno[2,3-b]- and thieno[3,2-b]thiophene-2-sulfonamides was prepared and evaluated for topical ocular hypotensive activity in glaucoma models. The 5-substituents were varied to maximize both inhibitory potency against carbonic anhydrase and water solubility. At the same time, these substituents were varied in order to obtain compounds with the appropriate pK(a) to minimize pigment binding in the iris. All of these variables were optimized in the best compound, 5-[[(methoxyethyl)](methoxyethyl)ethyl]amino]methyl]thieno[2,3-b] thiophene-2-sulfonamide hydrochloride (55).
Substituted thieno[3,2-b]thiophene-2-sulfonamides as topically active carbonic anhydrase inhibitors
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, (2008/06/13)
Novel substituted thieno[3,2-b]thiophene-2-sulfonamides are prepared by novel synthetic processes. These compounds are useful for the treatment of elevated intraocular pressure in compositions including ophthalmic drops and inserts.
