Global ETD Search
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Showing 1 to 20 of 23 for “"1,2,3-triazole"”.
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Pyrrolo[2,3-d]pyrimidine-based π-conjugated fluorophores with 1,2,3-triazole and ethynyl linkers: synthesis and photophysical properties /
… based oligoarylenes with ethynyl and 1,2,3-triazole linkers and to evaluate their photophysical properties. Novel chromophores - 2,4-bis(4-aryl-1,2,3-triazol-1-yl)pyrrolo[2,3-d]pyrimidines were prepared by CuAAC reaction. It was demonstrated that in the CuAAC reaction of …
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SÍNTESE DE NOVOS POTENCIAIS ANTAGONISTAS DO NMDA SUBTIPO NR2B DO SISTEMA NERVOSO CENTRAL BASEADOS EM CARBOXAMIDAS TRIAZÓLICAS
… of new amines and amides 1,2,3 - and 1,2,4 - triazoles, which were viewed as intermediates in the syntheses of new amino carboxamides with potentials antagonistic activities of the N-methyl-D-aspartate in the central nervous system. While the 3-amine-5-trifluoromethyl-2H-1,2,4-triazole (2) was …
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Design, Synthesis and Biological Evaluation of Novel Estradiol-Triazole Analogs Targeting Epidermal Growth Factor Receptors in Colorectal Cancer
… Additionally, pharmacophores such as 1,2,3-triazole showed potency towards many diseases including cancer. Therefore, incorporation of 1,2,3-triazole on a carrier such as estradiol could lead to novel analogs in drug discovery for treatment of cancer. A library of 800 compound containing …
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Design and Synthesis of CB1 Receptor Ligands and Synthesis of Amphibian Alkaloids
… the CB1 affinity for the 1,5-diaryl-1,2,3- triazole esters, a series of 4,5-diaryl-1-substituted-1,2,3-triazole analogues and a series of 4,5- diaryl-2-substituted-1,2,3-triazoles. Our research group has been interested in the synthesis of amphibian alkaloids due to their interesting …
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Development of biotin protein ligase inhibitors from Staphylococcus aureus as new antibiotics
… over the mammalian equivalent using 1,2,3-triazole and acylsulfonamide isosteres to replace the phosphoroanhydride linker found in biotinyl-5’-AMP 1.03. Chapter one describes the structure and catalytic mechanism of the target enzyme SaBPL, along with an overview of chemical analogues of …
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Design, Synthesis and Biological Evaluation of Novel Cannabinoid Antagonist
… target was to incorporate a bioisosteric 1,2,3-triazole ring into the vicinal diaryl group revealed in the prototypical antagonist/inverse agonist SR141716 (Rimonabant) that was presumed to interact with a unique region in the CB1 receptors. Based on our preliminary results we identified a …
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1,2,3-triazoles as X-factor in gold(I) activation of challenging C-C triple bond transformations
… which provides 1,4-disubstituted 1,2,3-triazoles has been reported in 2001. New method for highly funtionalized 1,2,3-triazole synthesis becomes very desirable along with the discovery of unique properties of this heterocyclic structure. Our group focused on the synthesis of functional …
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STUDY OF CLICK CHEMISTRY: WORKING TOWARDS ‘CLICKING’ A NON-STEROIDAL ANTI-INFLAMMATORY TO AN APOPTOSIS INHIBITOR Q-VD-OPH
The exploitation of the copper(I)-catalyzed 1,2,3-triazole forming reaction between azides and terminal alkynes has contributed to drug discovery due to the high degree of dependability, efficiency, specificity and biocompatibility of the reactions and products. Using this well-known click …
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Investigations into the Manipulation of 1,2,3-Triazoles and Towards an Asymmetric ‘Click’ Reaction of Meso Bis-Alkynes
… undertaken to generate various substituted 1,2,3-triazoles and a small group of bis alkyne-containing compounds, followed by their attempted application in an asymmetric ‘click’ reaction. The first chapter gives an outline to the importance of desymmetrization within organic synthesis, providing …
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An Exploratory Study of the Effects of BIS-Substituted Triazolium Bromide Salts on the Proliferation of WI-38 Lung Cells and H-1299 Lung Cancer Cells
… biological activity of the salts, Dibenzyl-benzotriazole (BT 1-1), Bis(2-Naph) Benzotriazole (BT 2-2), 2-Naph QuinBenzotriazole (BT 2-3), Bis-Naphthylacylbenzotriazole (BT 4-4), BisNaphAcyl - 1,2,3-triazole (T3 4-4) and Bis-3-phenylbenzyl-1,2,3- triazole (T3 5-5), on normal lung cells (WI-38), …
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Synthetic and computational investigations into reaction pathways towards complex heterocyclic ring systems
… hexahydropyrrolo-[2,3-d]-1,2,3-triazole. One of our main aims was to synthesise novel 1,2,3,5-tetrazocines that possessed three phenyl and one methyl group(s) attached to the eight-membered ring, as previously synthesised 1,2,3,5-tetrazocines are of the tetra-phenyl variety. …
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Pirolo[2,3-d]pirimidino π-konjuguotų fluoroforų, turinčių 1,2,3-triazolo ir etinil jungtukus, sintezė ir fotofizikinės savybės /
… based oligoarylenes with ethynyl and 1,2,3-triazole linkers and to evaluate their photophysical properties. Novel chromophores - 2,4-bis(4-aryl-1,2,3-triazol-1-yl)pyrrolo[2,3-d]pyrimidines were prepared by CuAAC reaction. It was demonstrated that in the CuAAC reaction of …
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Amine Nucleophilic Addition to Nitro-alkene as a New Reaction Mode for the Synthesis of N-heterocycles
… 100% chirality retention.;Unique Reactivity of Triazole Gold towards Alkyne Activation to Enones and Chiral Allenes: 1,2,3-Triazole coordinated gold(I) complexes were found as the effective catalysts in promoting propargylic ester/ether rearrangement and sequential allene hydration giving enones …
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Synthesis of oligonucleotide analogues for use in DNA nanostructures
… opposite<br/>terminal alkyne, to produce a 1,2,3-triazole linkage between the two reactants. The<br/>catenane was characterised by denaturing polyacrylamide gel electrophoresis, UV<br/>melting studies and enzyme digestion.
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Ligand and Protein Dynamics of CYP3A4
… ligand binding for three small molecules (1,2,3-triazole, imidazole, and cyanide) binding to CYP3A4 is characterized via UV/Vis stopped-flow spectroscopy using the analytical approach described in Chapter 3. Assignment of a ligand binding mechanism to kinetic data provides an indirect measure of …
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Boron Functionalization of BODIPY Dyes, and Their Evaluation as Bioimaging Agents
… 4 represents the investigation of six 1,2,3-triazole-BODIPYs under the Cu(I)-catalyzed Huisgen cycloaddition reaction conditions. A novel BODIPY bearing a chiral moiety was synthesized using method C and X-ray crystallography confirmed its identity. Chapter 5 reports the synthesis of …
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The α-helical conformation of polypeptides: design, regulation, and applications
… bonding interactions. Specifically, 1,2,3-triazole groups were incorporated on the side chains of polypeptides, which serve as both hydrogen bond donors and acceptors at neutral and basic pH to disrupt the α-helical structure, while lose their disrupting ability when protonated at acidic pH …
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Design and synthesis of components for optically active metal-organic frameworks (MOFs) and synthetic routes to diverse deuterium labelled α-diazoacetates, α-diazoacetamides, α-diazoketones, and the antibiotic azaserine
… (S)-BINOL-derived building blocks bearing 1,2,3-triazole moieties is described. Secondary functional groups can undergo post-synthetic modification resulting in the introduction of a catalytically active site. Within this research project an effective method for purification of commercially …
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QUANTITATIVE PROTEOMIC APPROACHES TO STUDY DRUG MECHANISM OF ACTION
… group to generate a 1,4-disubstituted 1,2,3-triazole ring. In this way, it is possible to functionalize the inhibitor under development with an alkyne moiety that could be labelled with a fluorescent-azide for target engagement detection and quantitation in native environments and a …
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Quinoline-triazole half-sandwich iridium(III) complexes: Synthesis, antiplasmodial activity and preliminary transfer hydrogenation studies
… strains. Two series of 7-chloroquinoline-1,2,3-triazole ligands, one with the direct attachment of the triazole to the quinoline and one where the two entities are separated by an aminopropyl linker, were synthesised. Coordination of selected ligands with [IrCl(μ-Cl)(Cp*)]₂ yielded six neutral, …
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