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Showing 1 to 8 of 8 for “"Falcipain"”.
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Part A: Antimalarial agents modified at the C-16 position of artemisinin; Part B: Lead optimization of falcipain-2 and falcipain-3 inhibitors
… will be improved. Part B: Lead Optimization of Falcipain-2 and Falcipain-3 Inhibitors. The expanding usage of artemisinin combination therapy casts concern about the potential development of drug resistance to this drug family, thus the search for new drug targets is always needed. Falcipain-2 …
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Utilization of the Baylis-Hillman and related reactions in antiparasitic drug discovery
… of two parasitic cysteine proteases (cruzain and Falcipain-2) and as antiparasitic agents. The utilization of polymer-supported bases in the Baylis-Hillman reaction is described. The use of ultrasound in combination with Lewis acids is also described in an attempt to improve the reaction rate.
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Synthesis and Antimalarial evaluation of Gold Thiosemicarbazone Complexes and Polyamine-Thiosemicarbazone Dendrimers
… activity against the malarial cysteine protease (falcipain-2). In most cases gold complexes showed enhanced antiplasmodial activities relative to their corresponding ligands. However, no correlation was found between antiplasmodial activities and the inhibition of falcipain-2 in respect of studied …
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New aminoquinoline antimalarial cysteine protease inhibitors based on the isatin natural product scaffold
… compounds were tested against the enzyme falcipain-2 (Rec-FP-2) as well as the parasite source of this protease, Plasmodium Jalciparum (P.f. W2). The results of structure activity relationship studies demonstrate the influence of substituents at position 5 of the isatin scaffold. With …
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Synthese und Eigenschaften N-Acylierter Aziridin-2,3-dicarboxylate als selektive, peptidomimetische Inhibitoren von Cystein-Proteasen der Cathepsin-L-Subfamilie
… B (human), Cathepsin L (Paramecium tetraurelia), Falcipain-2 (Plasmodium falciparum) und Rhodesain (Trypanosoma brucei rhodesiense). Die Verbindungen sind als irreversible Inhibitoren der Proteasen konzipiert. Der Aziridin-Baustein als Elektrophil wird durch den Cystein-Rest des aktiven Zentrums …
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Synthese und Testung nichtpeptidischer Cystein-Protease-Inhibitoren - Etacrynsäure als Leitstruktur
… den Cystein-Proteasen Papain, Cathepsin B (CB), Falcipain (FP) und Rhodesain (RD) getestet. Gegen Serin-Proteasen wurde keine Hemmung festgestellt. Die meisten Inhibitoren zeigten bei CB, FP und RD eine nicht-zeitabhängige Kinetik der Enzyminaktivierung. Nur bei Papain wurde eine zeitabhängige …
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Novel Antimalarial and Antitubercular Agents Based on Natural Products
… that the isatin-chalcone hybrids inhibited falcipain-2 activity, whereas the thiolactone-chalcone hybrids were devoid of enzyme inhibitory activity. With regard to antitubercular activity, the advanced intermediates were more active than the hybrid constructs. The most promising …
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Use of Structure-And Ligand-Based Drug Design Tools for the Discovery of Small Molecule Inhibitors of Cysteine Proteases for the Treatment of Malaria and Sars Infection
… and hemoglobinase of P. falciparum , referred as Falcipains (FPs), by the structure-based virtual screening of the focused libraries enriched in soft-electrophiles containing compounds. Twenty one diverse, non-peptidic, low micromolar hits were identified. A combined data mining and combinatorial …