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 18 of 18 for “"Antimycobacterial Agents"”.
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Design and Synthesis of Antimycobacterial Agents
Antibiotics have revolutionised modern life, however growing antimicrobial resistance threatens the advantages we have become accustomed to. Since the Golden Age of antibiotic drug discovery in the mid-20th century, progress has been tepid with target-based screens of synthetic and structurally …
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Discovery of Natural Product-based Antimycobacterial Agents Effective against Non-replicating Bacilli
<p>New antimycobacterial molecules that kill non-replicating Mycobacterium tuberculosis (Mtb) were identified by screening libraries of synthetic natural products. De novo screening of a 400-membered library of aurachin RE analogs resulted in discovery of UT-317 ((R)-20). UT-317 is a selective …
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Optimization of N-(1-Adamantyl)-3-Aryl Acetamides as Novel Antimycobacterial Agents
… event profiles of current treatment options, new antimycobacterial agents with novel mechanisms of action are direly needed. Mycobacteria membrane protein large 3 (MmpL3) is a transmembrane protein responsible for shuttling mycolic acids from the cytosol to the outer membrane of mycobacteria, and …
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Design, Synthesis, and Evaluation of Novel Antimycobacterial Agents With Enhanced Pharmacokinetic Profiles
… ineffective. Therefore, novel anti-TB and -NTM agents with greater efficacy and shorter treatment times are the need of the hour. One of the common drug targets for antibiotic intervention is the inhibition of bacterial cell wall biosynthesis. Mycolic acids, which are α-alkylated β-hydroxylated …
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Synthesis, characterisation, structure-activity and structure-property relationship studies of quinazolinones as antimycobacterial agents
… 2-aminoquinazolinones with promising antimycobacterial activity were identified from previous work in our research group. However, low aqueous solubility was associated with this series of compounds as a major liability, which needed to be addressed given its likely negative impact on …
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Synthesis, characterisation and pharmacological evaluation of silicon-containing aminoquinoline organometallic complexes as antiplasmodial, antitumor and antimycobacterial agents
… as ferroquine, KP1019 and NAMI-A, as therapeutic agents for the treatment of different diseases, the field of novel pharmacological transition metal agents continues to evolve. The constant increase in drug resistance and various undesirable side effects of current available therapies has led to …
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Design, synthesis, and biological evaluation of Antimycobacterial agents from plant derived Betulinic acid, Oleanolic acid and their derivatives
Tuberculosis (TB) is a dangerous disease that has killed several millions of people globally in recent times. The available drugs for the treatment of the disease are not effective for complete cure and in most cases, usually come with side effects, as a result of which new set of potent drugs are …
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The application of the Multi-Component Reaction (MCR) strategy in the design and synthesis of new antiplasmodial and antimycobacterial agents
… which exhibit in vitro antiplasmodial and antimycobacterial activity.
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In vitro metabolism of tetrazole aminoquinolines and derivatives of metergoline and fusidic acid
… fusidic acid as potential antiplasmodial and/or antimycobacterial agents.
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Synthesis, structure-activity relationship and solubility profiling of antimycobacterial aminoquinazolinones
… there is therefore a need to develop novel antimycobacterial agents to address these limitations. Within this context, 2-aminoquinazolinone compounds with potent antimycobacterial activity were previously identified. Poor solubility was recognized as a major issue requiring improvement. To …
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Semi-synthesis and evaluation of fusidic acid derivatives as potential antituberculosis agents
… acid has also been reported to possess in vitro antimycobacterial activity but was subsequently found to lack in vivo efficacy in a mouse model. Towards contributing to new antimycobacterial agents, this study focusses on repositioning fusidic acid for tuberculosis by employing prodrug and …
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Mycobacterium tuberculosis metallomics
… role of metal-based nanoparticles as potential antimycobacterial agents. Superparamagnetic iron oxide nanoparticles (SPIONs) were synthesised via co-precipitation of ferric chloride and ferric sulphate. The SPIONs were subsequently surface modified with secondary metals (Ag, Au, Cu, Ni) to …
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Anti-tubercular Clofazimine Analogs with Improved Physicochemical Properties
… approaches that require the use of multiple antimycobacterial agents for extended periods of time. Furthermore, the emergence of the drug-resistant strains has complicated the problem with approximately 190,000 deaths attributed to multidrug-resistant TB (MDR-TB) in 2014. There is a crucial …
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Design, synthesis and biological evaluation of verapamil analogues, reversed isoniazids and hybrid efflux pump inhibitors against Mycobacterium tuberculosis
… pre-existing role of rescuing the Mtb from toxic agents. These EPs extrude structurally unrelated compounds from the cell including anti-TB drugs and reduce the drug concentration to sub-inhibitory levels and aid Mtb in developing resistance. Therefore, development of antimycobacterials that …
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Isolation and identification of Naphthoquinones from Euclea natalensis with activity against Mycobacterium tubercolosis, other pathogenic bacteria and Herpes simplex virus
The antimycobacterial activity of twenty South African medicinal plants were investigated using two methods commonly used; the conventional agar plate method and the BACTEC radiometric method. Fourteen of the twenty acetone extracts of medicinal plants used to treat pulmonary diseases showed …
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Variability in the pharmacokinetics of rifapentine in South African tuberculosis patients : a classical and population approach
… largely on a limited number of chemotherapeutic agents, most of which have been used for the past 30 years. Discovery and development of new antimycobacterial agents has been relatively stagnant. New impetus from the Global Alliance for Tuberculosis Drug Development aims to register a new …
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Isolation and characterization of African marine natural products and repositioning of the natural product antibiotic fusidic acid and privileged benzimidazole scaffold for tuberculosis and malaria
… malaria parasite Plasmodium falciparum. Good antimycobacterial activity (MIC90 10 µM) was observed in the analogues, which possessed bulky and/or polar substituents in close proximity to the amide bond. Moreover, hydrophilic electron-withdrawing substituents seem to enhance antimycobacterial …