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 20 of 35 for “"Aminoquinoline"”.
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Expanding the versatility of aminoquinoline organometallic complexes as anticancer and antibacterial agents
… photophysical and biological properties. The aminoquinoline motif has been recognised as a remarkably versatile pharmacophore owing to its paramount contribution in the clinical success of the historical antimalarial drug, chloroquine. On account of its inherent and ubiquitous biological …
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New aminoquinoline antimalarial cysteine protease inhibitors based on the isatin natural product scaffold
… need to discover 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 …
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Anti-cancer and anti-malarial 4-aminoquinoline derivatives : synthesis and solid-state investigations
… clinically established antimalarials, the 4-aminoquinolines haveproven to be the most significant and efficacious for the treatment and prophylaxis of malaria. However, their efficacy has decreased by the spread of drug resistant strains of the causative agent Plasmodium Jalciparum. Future …
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Application of IR and NMR spectroscopy to certain complexes of 8-hydroxyquinoline and 8-aminoquinoline
… IR spectra of a series of -tris, bis and mono(8-aminoquinoline) complexes of the first transition row metal(II) perchlorates and halides is reported.
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Synthesis, characterisation and pharmacological evaluation of silicon-containing aminoquinoline organometallic complexes as antiplasmodial, antitumor and antimycobacterial agents
… condensation reaction. Two silicon-containing aminoquinoline ligands 2.1 and 2.2 were derived from chloroquine, modified in the lateral side chain with organosilicon moieties. Compounds 2.1 and 2.2 were further reacted with dinuclear halfsandwich transition metal precursors [Ru(Ar)(µ-Cl)Cl]i …
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Development of aminoquinoline-benzimidazole hybrids and their organometallic complexes as antimicrobial agents against Plasmodium falciparum and Mycobacterium tuberculosis
… properties of new organic and ferrocenyl aminoquinoline-benzimidazole hybrid compounds, as well as the corresponding Platinum Group Metal (PGM)-containing complexes. The compounds were screened for their activity against Plasmodium falciparum, and for their cytotoxicity against the Chinese …
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Synthesis, antimalarial evaluation, Ç-hematin inhibition, and in silico and in vitro ADMET profiling of 4-aminoquinoline-hydroxypyridinone hybrids
… to fight drug resistant malaria parasites, 4-aminoquinoline-3,4-hydroxypyridinone hybrids were designed and synthesized. Their hypothesized mode of action was studied with respect to inhibition of hemozoin formation.
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Synthesis and investigation of quinoline based ß-haematin formation inhibitors as potential antimalarials
… or not replacing the 7-chloro group in the 4-aminoquinoline moiety with an electron withdrawing and hydrophilic substituent results in retention of antiplasmodial activity in the 4-aminoquinoline class of compounds was investigated...
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Haemozoin formation, effects of chloroquine on iron distribution in Plasmodium falciparum and the correlation of thermordynamic and structural factors with 4-aminoquinoline activity
An interfacial method was developed in order to investigate the role lipids might play in haemozoin biosynthesis. Infrared and X-ray diffraction measurements demonstrated that β-haematin, a synthetic counterpart of haemozoin, forms efficiently at pentanol/water, octanol/water and lipid/water …
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Bioactive chloroquine-based ligands and their gold complexes as potential novel antimalarial agents
Chloroquine(CO)-derived 4-aminoquinolines have proven to be the most efficacious antimalarial drugs for both the treatment and prophylaxis of malaria. However, with the advent of drug resistance, their ability to treat the disease has been significantly hindered. Future research into the synthesis …
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Antimalarial drug rescue through safety improvement: design, synthesis and evaluation of amaodiaquine analogues
… was to design and synthesize analogues of the 4-aminoquinoline drug amodiaquine with potentially improved safety and efficacy profiles using prior knowledge of the drug metabolism and pharmacokinetics (DMPK), toxicity and efficacy profile of the drug. A representative set of compounds in four …
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Characterisation of novel alpha1-adrenoceptor ligands
… for the α1A-AR over the 5-HT1A-R. Homobivalent 4-aminoquinoline compounds with increasing carbon linker lengths (C2-C12) were examined for α1A-AR selectivity. C2 and C9 provided the optimal linker length to achieve the highest affinity among this series of compounds. C2 to C6 and C12 showed …
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INVESTIGATIONS IN IRON, COPPER, AND PALLADIUM –CATALYZED C-H BOND FUNCTIONALIZATION
… of sp2 C-H bonds have been developed. Using 8-aminoquinoline auxiliary and copper catalyst, ortho C-H bonds of benzoic acid amides can be sulfenylated by disulfides. The method provides an alternative, milder way for the preparation of aryl trifluoromethylsulfides. Furthermore, ortho C-H bonds …
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Synthesis and evaluation of hybrid compounds based on antimalarial and anticancer pharmacophores
… synthesis and biological evaluation of chromone-aminoquinoline hybrids as potentially new chemotherapeutic agents.
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In vitro metabolism of tetrazole aminoquinolines and derivatives of metergoline and fusidic acid
… work conducted during the early development of aminoquinoline tetrazoles, and derivatives of metergoline and fusidic acid as potential antiplasmodial and/or antimycobacterial agents.
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Applications of ROMP Polymers
… of analytes. And we found analytes pairs: 5-aminoquinoline and EA9A, 8-aminoquinoline and 1-naphthylamine, can use the SPPs for tunable separations. Thus these SPPs demonstrate the tunable separation abilities with analytes mixture solutions.</p> <p>The second project is the synthesis of well …
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Synthesis and Physical Properties of Helical Nanosized Quinoline-based Foldamers: Structure, dynamics and photoinduced electron transport
… units) were successfully prepared based on 8-aminoquinoline-2-carboxylic acid monomer. The dynamic properties in gas phase and solution were investigated. Ion mobility mass spectrometry afforded access to the conformation state of foldamers in gas phase; DOSY and fluorescence anisotropy …
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