16588-18-4Relevant academic research and scientific papers
Antituberculosis agents bearing the 1,2-disubstituted benzimidazole scaffold
Yeong, Keng Yoon,Ang, Chee Wei,Ali, Mohamed Ashraf,Osman, Hasnah,Tan, Soo Choon
, p. 770 - 778 (2017/03/06)
Abstract: The emergence of drug-resistant strains in recent years has fueled the epidemic of tuberculosis. This necessitates the development of new chemical scaffolds to curb resistant tuberculosis for effective control of this disease. In this study, we have designed and synthesized two series of benzimidazole derivatives. Their antimycobacterial activities were initially evaluated using Mycobacterium tuberculosis H37RV strains. The most potent analog (6h) was further assessed using various drug-resistant M. tuberculosis strains. This report described the importance of benzimidazoles as new antitmycobacterial agents targeting both the M. tuberculosis H37RV as well as the drug-resistant-tuberculosis strains. The trifluoromethyl group which was essential for antimycobacterial activity was also highlighted. Graphical Abstract: Two series of benzimidazole derivatives and their antimycobacterial activities were evaluated using M. tuberculosis H37RV (MTB-H37RV) strains. Compound 6h was identified as the most potent among all synthesized compounds. The most potent analog was further assessed using various drug-resistant MTB strains. In addition, the trifluoromethyl was identified as an important substitution in giving good antimycobacterial effect. [InlineMediaObject not available: see fulltext.]
Structural Modifications of Benzimidazoles via Multi-Step Synthesis and Their Impact on Sirtuin-Inhibitory Activity
Yoon, Yeong Keng,Choon, Tan Soo
, p. 1 - 8 (2016/01/29)
Benzimidazole derivatives have been shown to possess sirtuin-inhibitory activity. In the continuous search for potent sirtuin inhibitors, systematic changes on the terminal benzene ring were performed on previously identified benzimidazole-based sirtuin i
Benzimidazoles as new scaffold of sirtuin inhibitors: Green synthesis, in vitro studies, molecular docking analysis and evaluation of their anti-cancer properties
Yoon, Yeong Keng,Ali, Mohamed Ashraf,Wei, Ang Chee,Shirazi, Amir Nasrolahi,Parang, Keykavous,Choon, Tan Soo
, p. 448 - 454 (2014/07/21)
Two series of novel benzimidazole derivatives were designed, synthesized and evaluated for their SIRT1 and SIRT2 inhibitory activity. Among the newly synthesized compounds, compound 4j displayed the best inhibitory activity for SIRT1 (IC50 = 54
Simple NIR complexes and their applicability in dye-sensitized solar cells
Neuthe,Popeney,Bialecka,Hinsch,Sokolowski,Veurmann,Haag
supporting information, p. 583 - 587 (2014/08/18)
Novel nickel(II)benzo-diimino-semiquinonate and palladium(II)benzo-imino- semiquinonate complexes were synthesized, tested regarding their applicability in dye sensitized solar cells, and characterized optically and electrochemically. All the dyes showed a strong absorption in the near infrared region. Various electron-withdrawing substituents were introduced into the complex ligands and evaluated with respect to the effect on the energy level of the frontier molecular orbitals. Energetically suitable complexes were then tested in TiO2 based dye-sensitized solar cells with different iodide-based electrolytes. Two of them exhibited energy conversion abilities suggesting their candidacy as co-sensitizers to known visible light-absorbing dyes in order to extend the spectral window used for light harvesting into the infrared region to increase the total conversion efficiency of the cell.
Ferrostatins inhibit oxidative lipid damage and cell death in diverse disease models
Skouta, Rachid,Dixon, Scott J.,Wang, Jianlin,Dunn, Denise E.,Orman, Marina,Shimada, Kenichi,Rosenberg, Paul A.,Lo, Donald C.,Weinberg, Joel M.,Linkermann, Andreas,Stockwell, Brent R.
supporting information, p. 4551 - 4556 (2014/04/17)
Ferrostatin-1 (Fer-1) inhibits ferroptosis, a form of regulated, oxidative, nonapoptotic cell death. We found that Fer-1 inhibited cell death in cellular models of Huntington's disease (HD), periventricular leukomalacia (PVL), and kidney dysfunction; Fer-1 inhibited lipid peroxidation, but not mitochondrial reactive oxygen species formation or lysosomal membrane permeability. We developed a mechanistic model to explain the activity of Fer-1, which guided the development of ferrostatins with improved properties. These studies suggest numerous therapeutic uses for ferrostatins, and that lipid peroxidation mediates diverse disease phenotypes.
COMPOUNDS, COMPOSITIONS, AND METHODS FOR MODULATING FERROPTOSIS AND TREATING EXCITOTOXIC DISORDERS
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Paragraph 0173; 0180; 0188, (2013/10/22)
The present invention provides, inter alia, a compound having the structure: (Formula (I). Also provided are compositions containing a pharmaceutically acceptable carrier and a compound according to the present invention. Further provided are methods for treating or ameliorating the effects of an excitotoxic disorder in a subject, methods of modulating ferroptosis in a subject, methods of reducing reactive oxygen species (ROS) in a cell, and methods for treating or ameliorating the effects of a neurodegenerative disease.
