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Search for "high throughput" in Full Text gives 97 result(s) in Beilstein Journal of Organic Chemistry.
Chemical–biological characterization of a cruzain inhibitor reveals a second target and a mammalian off-target
Beilstein J. Org. Chem. 2013, 9, 15–25, doi:10.3762/bjoc.9.3
- compound concentrations required to reduce parasite numbers in C2C12 host cells by 90% as compared to untreated controls, as determined by using a high-content imaging-based screening (HCS) approach [33][40]. This high-throughput assay provides a rapid measure of the initial acute effects of test compound
Automated three-component synthesis of a library of γ-lactams
Beilstein J. Org. Chem. 2012, 8, 1804–1813, doi:10.3762/bjoc.8.206
- ; maleimide; organocatalysis; parallel synthesis; reductive amination; Introduction In recent years, the rapid access to structurally diverse and complex small molecules has grown in importance within the context of high-throughput screening of biologically relevant targets. The need for such compounds, both
Exploring chemical diversity via a modular reaction pairing strategy
Beilstein J. Org. Chem. 2012, 8, 1293–1302, doi:10.3762/bjoc.8.147
- demonstrate interesting behavior in biological screening. To gauge these prospects rigorously, these compounds have been submitted for evaluation of their biological activity in high-throughput screening assays at the NIH MLPCN and the results will be reported in due course. Biologically active benzofused
Design of a novel tryptophan-rich membrane-active antimicrobial peptide from the membrane-proximal region of the HIV glycoprotein, gp41
Beilstein J. Org. Chem. 2012, 8, 1172–1184, doi:10.3762/bjoc.8.130
- , ranging from diverse peptides isolated from different natural sources to synthetic peptides generated with high-throughput screening methods. From this large sample size, a number of characteristics have been identified that all contribute to the antimicrobial potency of these polypeptides. In this study
Synthesis of a library of tricyclic azepinoisoindolinones
Beilstein J. Org. Chem. 2012, 8, 1091–1097, doi:10.3762/bjoc.8.120
- synthesis was achieved by a subsequent alkene epoxidation and zinc-mediated aminolysis reaction. The resulting library products provided selective hits among a large number of high-throughput screens reported in PubChem, thus illustrating the utility of the novel scaffold. Keywords: chemical diversity
Synthesis and in silico screening of a library of β-carboline-containing compounds
Beilstein J. Org. Chem. 2012, 8, 1048–1058, doi:10.3762/bjoc.8.117
- maximally diverse chemical space. The synthesis of a modified subset of this virtual compound library is described within, where modifications were mainly driven by studies of compound stability. Furthermore, a high throughput, in silico screening analysis of this library identified a number of potential
- predict potential targets of the newly synthesized library of β-carboline-containing compounds. High-throughput docking studies for protein-target prediction of newly synthesized compounds Molecular docking studies were performed with the 34 newly synthesized compounds, represented by scaffolds 1, 2, 3
- . Conclusion A library of 34 β-carboline-containing compounds was synthesized utilizing a skeletal diversification strategy. High-throughput docking and ligand-based protocols were implemented to predict potential biological targets of the newly synthesized β-carbolines. The docking approach uses a structure
Parallel solid-phase synthesis of diaryltriazoles
Beilstein J. Org. Chem. 2012, 8, 1027–1036, doi:10.3762/bjoc.8.115
- method may find application in the combinatorial search for selective protein–protein inhibitors. To that end, most of the compounds prepared herein were submitted to the Molecular Libraries Small Molecular Repository for ongoing inclusion in high-throughput screening activities. Experimental General
The use of glycoinformatics in glycochemistry
Beilstein J. Org. Chem. 2012, 8, 915–929, doi:10.3762/bjoc.8.104
- topologies are computed to match the experimentally determined data [149]. GlyQuest [139] and GlycoMiner [131] are designed for high-throughput analysis of glycopeptides that carry N-glycan chains. Glyco-Peakfinder [133] and GlycoWorkbench [138] cover the complete workflow from recorded experimental data to
Formation of carbohydrate-functionalised polystyrene and glass slides and their analysis by MALDI-TOF MS
Beilstein J. Org. Chem. 2012, 8, 753–762, doi:10.3762/bjoc.8.86
- ; Introduction Microarrays have become valuable tools in the high-throughput analysis of biological interactions and have promising applications for the development of diagnostic devices in clinical environments [1]. The initial success with DNA microarrays has prompted investigations into other biomolecular
- analysis. The matrix is typically cocrystallised with the sample, which can lead to irregular surfaces, which can be a problem for reproducible analysis, especially when used in array format as a high-throughput tool. To avoid the use of such a matrix, we were interested in investigating trityl
Investigation of the network of preferred interactions in an artificial coiled-coil association using the peptide array technique
Beilstein J. Org. Chem. 2012, 8, 640–649, doi:10.3762/bjoc.8.71
- association between artificial and natural patterns by means of SPOT technology, which is a simple high-throughput method shown to be useful for the characterization of intermolecular domains in general and coiled coils in particular at the amino-acid level [12][13][14][15]. This method assisted in the
Synthetic approaches to multifunctional indenes
Beilstein J. Org. Chem. 2011, 7, 1739–1744, doi:10.3762/bjoc.7.204
- careful column chromatography, and sometimes a high-throughput flash purification system was necessary. The structures of the new compounds were confirmed by spectroscopic methods, and their 1H NMR and 13C NMR chemical shifts and physical data are gathered in the experimental description (Supporting
Highly efficient cyclosarin degradation mediated by a β-cyclodextrin derivative containing an oxime-derived substituent
Beilstein J. Org. Chem. 2011, 7, 1543–1554, doi:10.3762/bjoc.7.182
- effect of this OP on AChE was estimated by using a fully automated high-throughput screening assay recently developed for the characterization of potential nerve agent detoxifying materials [43]. This test involves incubation of the nerve agent with an excess of a respective cyclodextrin derivative at
Chimeric self-sufficient P450cam-RhFRed biocatalysts with broad substrate scope
Beilstein J. Org. Chem. 2011, 7, 1494–1498, doi:10.3762/bjoc.7.173
- high-throughput screening protocol for evaluating chimeric, self-sufficient P450 biocatalysts and their mutants against a panel of substrates was developed, leading to the identification of a number of novel biooxidation activities. Keywords: biocatalysis; C–H activation; high-throughput screening
- , often with high regio- and stereoselectivity [1], and are therefore attractive candidates for biocatalyst development. However, the need for reconstitution of protein redox partners, the necessary use of expensive NAD(P)H, and the lack of widely applicable high-throughput screening protocols render the
- whole-cell P450 systems would be amenable to incorporation into a high-throughput screening protocol in multiwell plates. Figure 1 outlines the design of the screening platform: E.coli hosts containing a variety of easily engineered chimeric constructs are incubated with the substrate under
Evaluation of a commercial packed bed flow hydrogenator for reaction screening, optimization, and synthesis
Beilstein J. Org. Chem. 2011, 7, 1141–1149, doi:10.3762/bjoc.7.132
- from ThalesNano. These cartridges consist of a solid catalyst contained within stainless steel tubes fitted with thin 8 micron frits. The manufacturer also demonstrated that high-throughput synthesis can be facilitated on the H-Cube® using a Tecan liquid handler for automated sample injection and
Multicomponent synthesis of artificial nucleases and their RNase and DNase activity
Beilstein J. Org. Chem. 2011, 7, 1135–1140, doi:10.3762/bjoc.7.131
- especially important because multicomponent reactions (MCR) could be adapted to a high throughput synthesis of libraries of compounds. It is known that isocyanide-based MCR are very efficient for synthesis of peptides and peptide molecules [19][20][21][22][23][24]. We proposed that the desired compounds 5
- -stranded circular plasmid DNA, high-throughput RT-qPCR was developed and used. All synthesized compounds were shown to be able to cleave completely single-stranded RNA but not single-stranded cDNA or hybrid of RNA with cDNA after reverse transcription irrespective of the structure of their substituents and
Chiral gold(I) vs chiral silver complexes as catalysts for the enantioselective synthesis of the second generation GSK-hepatitis C virus inhibitor
Beilstein J. Org. Chem. 2011, 7, 988–996, doi:10.3762/bjoc.7.111
- evaluation, the compounds targeting HCV replication being the most promising candidates to achieve a sustained virological response [1][4]. Several years ago, a high-throughput screening of the GlaxoSmithKline compound collection identified a series of small pyrrolidine molecules, e.g., 1 (Figure 1), able to
Continuous flow hydrogenation using polysilane-supported palladium/alumina hybrid catalysts
Beilstein J. Org. Chem. 2011, 7, 735–739, doi:10.3762/bjoc.7.83
- polymer-incarcerated (PI) catalysts, which have high catalytic activity without causing metal leaching [1]. Heterogeneous catalytic hydrogenation in a batch system has recently been applied to continuous flow hydrogenation systems for high-throughput synthesis [2][3][4][5][6][7][8][9][10]. There are
An overview of the key routes to the best selling 5-membered ring heterocyclic pharmaceuticals
Beilstein J. Org. Chem. 2011, 7, 442–495, doi:10.3762/bjoc.7.57
Tandem catalysis of ring-closing metathesis/atom transfer radical reactions with homobimetallic ruthenium–arene complexes
Beilstein J. Org. Chem. 2010, 6, 1167–1173, doi:10.3762/bjoc.6.133
- (Scheme 2). This process, known as assisted tandem catalysis [6], presents significant advantages over multistep synthesis for increasing molecular complexity, particularly in terms of time- and cost-savings, atom economy, environmental friendliness, or applicability to diversity-oriented high-throughput
Asymmetric reactions in continuous flow
Beilstein J. Org. Chem. 2009, 5, No. 19, doi:10.3762/bjoc.5.19
- reproducibility due to the precise control over reaction conditions in these devices. Continuous flow technology has excellent potential for the integration of a high level of automation and for the incorporation of on-demand reaction analysis. This can be advantageous for applications such as high-throughput
Chemistry in flow systems
Beilstein J. Org. Chem. 2009, 5, No. 15, doi:10.3762/bjoc.5.15
- techniques that originate from high-throughput chemistry laboratories as they can be combined with the use of immobilized reagents or catalysts, or by using fixed bed reactors in parallel. These developments in flow techniques using mini and micro flow reactors have initiated changes that will pave the way
Mixtures of monodentate P-ligands as a means to control the diastereoselectivity in Rh-catalyzed hydrogenation of chiral alkenes
Beilstein J. Org. Chem. 2005, 1, No. 3, doi:10.1186/1860-5397-1-3
- libraries of chiral metal complexes or metal-free catalysts[9] followed by medium- or high-throughput screening.[5] Catalyst diversity is achieved by the design and synthesis of modular ligands comprised of several building blocks which can be varied at will and easily assembled covalently. Another strategy
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