Global ETD Search
Search theses and dissertations gathered from participating repositories worldwide. Every result links back to the library that holds it. No account is needed.
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Showing 1 to 17 of 17 for “"Isatin"”.
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Thiazolidinone-isatin hybrids as multi-target anticancer agents
… solid tumours. Therefore, considering that isatin and thiazolidinone could be considered as privileged scaffolds in medicinal chemistry and pursuing in our ongoing work on benzene sulphonamides isatin-thiazolidinone hybrids as inhibitors of hCA IX and hCA XII, four series of molecules were …
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New aminoquinoline antimalarial cysteine protease inhibitors based on the isatin natural product scaffold
… new antimalarial drugs. New 4-aminoquinoline isatin derivatives have been designed and synthesised. Isatin was used as a biologically validated starting point for the design of chemical libraries directed at the intended target due to its privileged nature. Included in the design of these …
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Synthesis and biological evaluation of antiparasitic Cysteine protease inhibitors based on the Isatin Scaffold
… project, a non-peptidic and low molecular weight isatin (indole-2, 3-dione) possessing a wide range of pharmacological properties was used as a scaffold to which different moeities were appended. Potential inhibitors of parasitic cysteine proteases and three strains of P. falciparum were …
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In silico-guided design, synthesis and antimicrobial activity of piperazine-linked 8-hydroxyquinoline-isatin hybrids
… for this study include 8-hydroxyquinoline and isatin. There exist reports on the versatility of the 8-hydroxyquinoline ring and the antimicrobial, anticancer, and antifungal activity ascribed to its derivatives, while the isatin scaffold known for rendering high hit rates, in targeted drug …
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Novel Antimalarial and Antitubercular Agents Based on Natural Products
… thiolactomycin, the non-peptidic natural product isatin and the chalcone scaffold. In this way a series of hybrids were constructed which can be subdivided into three main groups: (i) thiolactone-isatin hybrids, (ii) -amino alcohol thiolactone-chalcone and isatin-chalcone hybrids, and (iii) …
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The Oximes of 1-(3-Methoxy-4-Agetoxyphenyl)-2, 6-Dicarbethoxycyclohex-Anedione-3,5 and their Derivatives
… ketone consists of their condensation to isatin and isatin derivatives.
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Formation of Pyrroloindolines and Alkylation of N-heterocycles With Trichloroacetimidates and Synthesis of Quinoline Based Small Molecule Inhibitors of Ghrelin O-acyltransferase (goat)
… to effect the requisite transformations.</p><p>Isatin (1H-indol-2,3-dione) based structures are commonly found in molecules of medicinal interest. These molecules are usually synthesized in multiple steps, with their N-alkylation typically requiring the use of stoichiometric strong base which …
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Design, synthesis and evaluation of small molecules as inhibitors of plasminogen activator inhibitor-1
… para-chlorobenzyl, polyphenol, oxindole, or isatin-based units. By changing the architectural scheme of these compounds we hope to effectively change the potency of our inhibitors, and will be able to develop a structure-activity relationship that will allow us to design a more potent small …
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An investigation into the molecular mechanisms induced by derivatives of natural products in oesophageal cancer
… values. Novel halogenated artemisinin - isatin hybrid compounds displayed the best activity against oesophageal cancer cells, and were more potent than artesunate and dihydroartemisinin in a small panel of oesophageal, breast and cervical cancer cell lines tested. The novel derivatives …
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Catalytic promiscuity of two plant P450 enzymes: CYP725A4 from Taxus cuspidata and CYP71B102 from Isatis Tinctoria
… with 5-aminolevulinic acid supplementation and isatin hydrolase coexpression altogether increased indigo formation, while supplementation with isatin and 2-oxindole increased indirubin formation. The results of this study showed that the catalytic promiscuity of CYP725A4 and CYP71B102 could be …
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Trichloroacetimidates As Outstanding Electrophiles for the Carbon-nitrogen, Carbon-oxygen and Carbon-carbon Bonds Formation and Synthetic Studies of Protein Phosphatase-5 (pp5) Small Molecule Inhibitors
… carbocation precursors for new reactions.Isatin is an ambidentate nucleophile and commonly can be N-alkylated using harsh conditions and specialized reaction conditions, while O-alkylation is uncommon and has only been reported utilizing silver salts. These important structures can be …
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Exploring Nickel Catalysis in Carbonyl and Alcohol Addition Reactions
… For this purpose, pharmaceutically relevant isatin substrates are derivatized, providing access to substitution at the 3-position. Coupling isatins with aryl halides yields 3-aryl-3-hydroxy-2-oxindole products which are scaffolds for many natural product derivatives. Through high-throughput …
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Design and synthesis of new potential anticancer agents and high-selective A2B antagonists
… like cancer. Within this category, several isatin-thiazolinone-pyrazoline hybrids were synthesized. Some of them were submitted to biological assays, demonstrating good activity toward different solid tumour cell-lines. In the second class of compounds, the synthetic efforts were combined to …
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Enzymology And Medicinal Chemistry Of N5-Carboxyaminoimidazole Ribonucleotide Synthetase : A Novel Antibacterial Target
… inhibitors. These studies revealed that the isatin core of class II inhibitors is capable of undergoing photochemical conversion to isatoic anhydride. Once formed, the anhydride is capable of reacting with the protein. Treatment of N5-CAIR synthetase with the photoreactive agent lead to the …
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De Novo Design of secondary structures: Synthesis and conformational studies
… about the catalyzed aldol addition of acetone to isatins. By means of DFT and AIM calculations, the steric and stereoelectronic effects that control the enantioselectivity in the cross-aldol addition of acetone to isatin catalysed by L-proline have been studied, also in the presence of small …
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Exploration of Carbon-oxygen and Carbon-nitrogen Bond Formation Utilizing Trichloroacetimidates and Investigations of New Reactions Mediated By Oxoammonium Salts
… of alkenes with primary alcohols, water, and isatin was also initiated.</p>
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Estudo teórico conformacional da delta-toxina e teórico-experimental da interação de complexos de cobre-base de Schiff com o canal iônico da alfa-toxina de Staphylococcus aureus/
O Staphylococcus (S.) aureus é responsável por inúmeros casos de infecções em animais e seres humanos. Essa bactéria secreta uma grande variedade de exoproteínas, incluindo quatro hemolisinas: alfa, beta, gama e delta. A atividade hemolítica da alfa-toxina (α-HL) se deve a formação de poros em …