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Influence Of Conformational Restriction On The Antibacterial Activity And Ribosomal Selectivity Of Aminoglycoside Antibiotics, Michael Gabriel Pirrone
Influence Of Conformational Restriction On The Antibacterial Activity And Ribosomal Selectivity Of Aminoglycoside Antibiotics, Michael Gabriel Pirrone
Wayne State University Dissertations
The ever-increasing threat posed by multidrug-resistant infectious bacteria necessitates
the development of novel antibiotics. Aminoglycoside antibiotics are growing in interest due to
their broad spectrum of activity, lack of known drug related allergies, low manufacturing cost,
and their well-studied mechanism of action. The simplification of rational drug design due to the
well-studied mechanism of action is the key to overcoming the issues presented by these drugs,
namely ototoxicity and nephrotoxicity.
A study of the effect of the conformation of the aminoglycoside ring I side chain is
described wherein it was discovered that an increase in a particular conformation augments the …
Synthesis Of Apramycin And Paromomycin Derivatives As Potential Next Generation Aminoglycoside Antibiotics And Chemistry Of Isothiocyanato Sialyl Donors, Appi Reddy Mandhapati
Synthesis Of Apramycin And Paromomycin Derivatives As Potential Next Generation Aminoglycoside Antibiotics And Chemistry Of Isothiocyanato Sialyl Donors, Appi Reddy Mandhapati
Wayne State University Dissertations
AGAs are clinically important antibacterials for human therapy and have long been used as highly potent antibiotics for treating several bacterial infections. The fidelity of protein synthesis is affected by AGAs in the course of binding to specific sites of the bacterial rRNA. The clinical use of AGAs and their applications as therapeutics is restricted by toxicity (irreversible ototoxicity and reversible nephrotoxicity) and by the resistance of pathogens. The objective of this research was the development of proficient AGAs that are less toxic (i.e., more selective) and that evade resistance. The first three chapters of this thesis are aimed towards …