3538-68-9Relevant articles and documents
Hydrophobic derivatization of N-linked glycans for increased ion abundance in electrospray ionization mass spectrometry
Walker, S. Hunter,Lilley, Laura M.,Enamorado, Monica F.,Comins, Daniel L.,Muddiman, David C.
, p. 1309 - 1317 (2011)
A library of neutral, hydrophobic reagents was synthesized for use as derivatizing agents in order to increase the ion abundance of N-linked glycans in electrospray ionization mass spectrometry (ESI MS). The glycans are derivatized via hydrazone formation and are shown to increase the ion abundance of a glycan standard more than 4-fold. Additionally, the data show that the systematic addition of hydrophobic surface area to the reagent increases the glycan ion abundance, a property that can be further exploited in the analysis of glycans. The results of this study will direct the future synthesis of hydrophobic reagents for glycan analysis using the correlation between hydrophobicity and theoretical non-polar surface area calculation to facilitate the development of an optimum tag for glycan derivatization. The compatibility and advantages of this method are demonstrated by cleaving and derivatizing N-linked glycans from human plasma proteins. The ESI-MS signal for the tagged glycans are shown to be significantly more abundant, and the detection of negatively charged sialylated glycans is enhanced.
A combinatorial approach for the discovery of drug-like inhibitors of 15-lipoxygenase-1
van der Vlag, Ramon,Guo, Hao,Hapko, Uladzislau,Eleftheriadis, Nikolaos,Monjas, Leticia,Dekker, Frank J.,Hirsch, Anna K.H.
, p. 45 - 55 (2019/04/27)
Human 15-lipoxygenase-1 (15-LOX-1) is a mammalian lipoxygenase which plays an important regulatory role in several CNS and inflammatory lung diseases. To further explore the role of this enzyme in drug discovery, novel potent inhibitors with favorable phy
Synthesis of N′-propylhydrazide analogs of hydroxamic inhibitors of histone deacetylases (HDACs) and evaluation of their impact on activities of HDACs and replication of hepatitis C virus (HCV)
Kozlov, Maxim V.,Konduktorov, Konstantin A.,Shcherbakova, Anastasia S.,Kochetkov, Sergey N.
supporting information, p. 2369 - 2374 (2019/06/17)
N′-Propylhydrazide analogs of hydroxamic inhibitors of histone deacetylases (HDACs), including tubastatin A, vorinostat and belinostat, were synthesized. All prepared compounds inhibited HDAC1/2/3, but not HDAC6, except for one hydrazide analog of HDAC4/5/7 inhibitor that was completely inactive. A novel 4-substituted derivative of N′-propylbenzohydrazide with extremely high anti-HCV activity was discovered.