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Medicinal-Pharmaceutical Chemistry Commons

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Full-Text Articles in Medicinal-Pharmaceutical Chemistry

The Development Of Metallohydroxamates As Novel Anti-Bacterial And Anti-Leishmanial Agents, Donal Keogan Jul 2018

The Development Of Metallohydroxamates As Novel Anti-Bacterial And Anti-Leishmanial Agents, Donal Keogan

PhD theses

Since the initial development and clinical use of antibiotics, there has been a steady and alarming increase in the levels of antibiotic resistant bacterial infections arising worldwide. The reduced efficacy of antibiotics coupled to the lack of new classes of antibiotics being developed, may result in antibiotic resistance infections rising to epidemic levels.

The decrease in new antibiotic discovery has resulted in increased interest in repurposing and repositioning of previously developed drugs as effective anti-bacterial treatments. The use of metals in medicine is not a new phenomenon as they have been used in medicine for thousands of years. Nonetheless the ...


Real-Time Recording Of The Cellular Effects Of The Anion Transporter Prodigiosin., Shane Cheung, Dan Wu, Harrison C. Daly, Nathalie Busschaert, Marina Morgunova, Jeremy C. Simpson, Dimitri Scholz, Philip A. Gale, Donal F. O'Shea Apr 2018

Real-Time Recording Of The Cellular Effects Of The Anion Transporter Prodigiosin., Shane Cheung, Dan Wu, Harrison C. Daly, Nathalie Busschaert, Marina Morgunova, Jeremy C. Simpson, Dimitri Scholz, Philip A. Gale, Donal F. O'Shea

Chemistry Articles

The unraveling of the cellular effects of anion transporters is key to their potential development as apoptosis-inducing or autophagy-disrupting therapeutics. Here, we conducted a systematic study of the cellular responses to the anion transporter prodigiosin by using a pH on/off responsive near-infrared (NIR)-fluorescent probe in HeLa and LAMP1-GFP-transfected HeLa cell lines. The sequence of localized and global cellular acidity changes and the resulting outcomes induced by the anion transporter were visualized with high temporal and spatial resolution. The results show that prodigiosin causes the pH within the lysosomal lumen to rise, after which a non-organelle-specific increase in acidity ...


Development Of A Novel Carboplatin Like Cytoplasmic Trackable Near Infrared Fluorophore Conjugate Via Strain-Promoted Azide Alkyne Cycloaddition., Eolann Kitteringham, Dan Wu, Shane Cheung, Brendan Twamley, Donal F. O'Shea, Darren M. Griffith Feb 2018

Development Of A Novel Carboplatin Like Cytoplasmic Trackable Near Infrared Fluorophore Conjugate Via Strain-Promoted Azide Alkyne Cycloaddition., Eolann Kitteringham, Dan Wu, Shane Cheung, Brendan Twamley, Donal F. O'Shea, Darren M. Griffith

Chemistry Articles

The successful design and pre-clicked synthesis of a non-toxic and cytosol trackable carboplatin-like near infrared fluorophore conjugate via strain-promoted azide alkyne cycloaddition (SPAAC) is reported. Reaction of cis-[Pt(2-azidopropane-1,3-diamine)(cbdca)] (cbdca = cyclobutane-1,1-dicarboxylato) and a bicyclo[6.1.0]non-4-yne near-infrared (NIR) azadipyrromethene fluorophore gave the corresponding clicked Pt-Fluorophore conjugate. The X-ray crystal structure of cis-[Pt(2-azidopropane-1,3-diamine)(cbdca)] was determined featuring the azide on the bidentate 1,3-diaminopropane ligand. The Pt-fluorophore conjugate is the first example of a Pt conjugate clicked via strain-promoted azide alkyne cycloaddition (SPAAC) where the reactive azide handle is on the amine ...