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 15 of 15 for “"fusidic acid"”.
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Semi-synthesis and evaluation of fusidic acid derivatives as potential antituberculosis agents
… treat both sensitive and resistant forms of TB. Fusidic acid is a naturally occurring antibiotic used to treat Gram-positive bacterial infections. It has potent activity against S. aureus and is clinically used to treat mild to moderately severe skin and soft-tissue infections. The mode of action …
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In vitro metabolism of tetrazole aminoquinolines and derivatives of metergoline and fusidic acid
… tetrazoles, and derivatives of metergoline and fusidic acid as potential antiplasmodial and/or antimycobacterial agents.
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Analytical Studies Concerning the Stability of Betamethasone Valerate and Fusidic acid Hemihydrate in Topical Pharmaceutical Preparations
… drug substances betamethasone 17-valerate and fusidic acid hemihydrate in topical pharmaceutical formulations. In particular, the work concentrates on formulation factors affecting the intra-molecular isomerisation of betamethasone 17-valerate to 21-valerate in a developmental topical cream for …
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Development of novel compounds to improve the resistance profile and spectrum of activity of fusidic acid
… pathogens motivated us to investigate Fusidic Acid (FA), a Gram-positive-only antibiotic as a novel solution to combat these deadly pathogens. Herein, we report the development of FA-CP, the first analogue of FA with equipotent activity. FA-CP also shows an improvement in activity …
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Repositioning fusidic acid for tuberculosis: semi-synthesis of analogues and impact of mycobacterial biotransformation on antibiotic activity
… the therapeutic options for TB chemotherapy. Fusidic acid (FA), a natural product-derived antibiotic, has modest in vitro antimycobacterial activity. Through a multi-disciplinary approach combining aspects of chemistry and biology, this study investigated the pharmacological and …
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Developing methods to prioritize in vitro drug combinations against Mycobacterium tuberculosis: fusidic acid as potential combination partner with known antitubercular agents
… firstly, exploring mechanisms of synergy between fusidic acid (FSA), a natural product antibiotic, and current anti-TB agents and, secondly, characterizing antibiotic action by delineating bacteriostatic and bactericidal compounds.
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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
… sponge species, Halichondria sp. and Hymeniacidon sp., is also reported herein. The specimens were collected from the Prince Edwards Islands in the Southern Ocean in the vicinity of Antarctica. With the aim to investigate the chemical and biological properties of the secondary metabolites …
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Preclinical pharmacokinetic evaluation of novel antimalarial and antituberculosis drug leads
… absorption. Investigation of two novel fusidic acid C-3 ester prodrugs aimed at repositioning fusidic acid for tuberculosis, showed high concentrations of the rodent specific 3-epifusidic acid metabolite that greatly reduced exposure of fusidic acid in mice. Further organ distribution …
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A medicinal chemistry approach to drug repositioning in the treatment of tuberculosis and malaria
… of two drugs, the antibacterial agent fusidic acid and the antipsychotic agent metergoline, in TB and/or malaria via medicinal chemistry approaches. New semisynthetic derivatives of fusidic acid and metergoline were synthesized and evaluated for antimycobacterial activity against the …
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Ring distortion of the alkaloid sinomenine and novel prodrug approaches to broad-spectrum antibiotics
… relationship of Gram-positive only antibiotic fusidic acid. Chapter 2 discusses the ring distortion of the alkaloid sinomenine using the complexity-to-diversity (CtD) approach to generate 66 total compounds, which played a key role in identifying the 3-dimensionality parameter, globularity …
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Synthesis and translation of novel gram-negative antibacterial agents
… scale-up and in-vivo testing of a promising fusidic acid analogue, dubbed FA-Oxane. It was found to possess notable activity versus Mycobacterium tuberculosis (Mtb) in cell culture, as well as an improved pharmacokinetic profile in mice. A new synthetic route was devised to synthesize …
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Super-Resolution Force Spectroscopy for Revealing Sub-nucleotide Motion in Ribosomal Frameshifting and DNA Methylation
… “-2” frameshifting complexes in the presence of fusidic acid. We termed this new state as “-1*”, whose dissociation force was shifted by approximately half a nucleotide compared to the normal “-1” reading frame at the 5’-end of the mRNA. With this unprecedented force resolution, we were also able …
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Διερεύνηση λοιμώξεων από πηκτάση-αρνητικά στελέχη του γένους Staphylococcus σε ασθενείς με προσθετικά υλικά
… στα αντιμικροβιακά clindamycin, ciprofloxacin, fusidic acid, SXT και στις αμινογλυκοσίδες, ενώ τα στελέχη του τύπου b έφεραν συχνότερα το γονίδιο aap (p=0.049). Τα στελέχη S. haemolyticus παρουσίασαν μικρότερη γενετική ποικιλομορφία, με έναν κύριο PFGE τύπο (h), που περιελάμβανε 44/58 στελέχη …
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Investigating permeation of anti-mycobacterial agents in Mycobacterium tuberculosis and M. tuberculosis-infected macrophages in vitro as a model for early stage tuberculosis drug discovery
… The highly lipophilic natural product, fusidic acid (FA), its known human metabolite, 3-ketofusidic (3-ketoFA or GKFA37), and two C-3 alkyl esters (GKFA16 and GKFA17) as FA prodrugs were utilized in the study. In addition, another chemical class, the less lipophilic benzoxazole-based …