219685-46-8Relevant articles and documents
New nitric oxide-releasing indomethacin derivatives with 1,3-thiazolidine-4-one scaffold: Design, synthesis, in silico and in vitro studies
Sava, Alexandru,Buron, Frederic,Routier, Sylvain,Panainte, Alina,Bibire, Nela,Profire, Lenu?a
, (2021)
In this study we present design and synthesis of nineteen new nitric oxide-releasing indomethacin derivatives with 1,3-thiazolidine-4-one scaffold (NO-IND-TZDs) (6a–s), as a new safer and efficient multi-targets strategy for inflammatory diseases. The che
With tyrosine kinase inhibitory activity of 2 - indolone derivatives and its preparation method and application
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Paragraph 0085; 0086, (2017/07/01)
The invention discloses a 2-indolone derivative with tyrosine kinase inhibition activity, geometric isomers and medicinal salts thereof, and a preparation method and an application of the above compounds. Tyrosine kinase inhibition activity evaluation confirms that the derivative is a compound with good tyrosine kinase activity, so the derivative has potential antitumor activity, and can be used to prepare tumor disease prevention and treatment medicines (antitumor medicines) as an active component. The derivative provides research and enforcement foundation for tumor treatment, and has a wide application prospect.
Suppression of store overload-induced calcium release by hydroxylated metabolites of carvedilol
Malig, Thomas,Xiao, Zhichao,Chen, S.R. Wayne,Back, Thomas G.
, p. 149 - 153 (2015/12/18)
Carvedilol is a drug widely used in the treatment of heart failure and associated cardiac arrhythmias. A unique action of carvedilol is its suppression of store overload-induced calcium release (SOICR) through the cardiac ryanodine receptor (RyR2), which can trigger ventricular arrhythmias. Since the effects of carvedilol metabolites on SOICR have not yet been investigated, three carvedilol metabolites hydroxylated at the 3-, 4′ and 5′-positions were synthesized and assayed for SOICR inhibition in mutant HEK 293 cells expressing the RyR2 mutant R4496C. This cell line is especially prone to SOICR and calcium release through the defective RyR2 channel was measured with a calcium-sensitive fluorescent dye. These results revealed that the 3- and 4′-hydroxy derivatives are slightly more effective than carvedilol in suppressing SOICR, while the 5′-analog proved slightly less active. Metabolic deactivation of carvedilol via these hydroxylation pathways is therefore insignificant.
