Murray State University

Poster Title

Synthesis of Amidopyrroles as Probes of Type 3 Aminoglycoside Kinases

Institution

Murray State University

Abstract

Aminoglycosides are antibiotics that were first identified in the mid 1940’s and have been widely used to treat bacterial infections. These antibiotic agents bind to important cellular components to disrupt bacterial growth and cause cell death. Because of overuse, bacteria have developed methods to destroy the effectiveness of these antibiotics. One common method involves the addition of a chemical group that modifies the antibiotic. To eliminate this particular mode of antibiotic resistance, the chemical modification site must be thoroughly investigated. To this end, groups of diverse compounds must be prepared to obtain data for use in Structure-Activity Relationship (SAR) studies. To obtain these groups, a common structure is identified as a scaffold from which a variety of new compounds can be made quickly, efficiently, and cost effectively. The resultant groups of compounds, or libraries, contain diverse structural components that can be used to systematically investigate the molecular interactions involved within a specific binding site. The synthesis of two series of amidopyrroles are presented.

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Synthesis of Amidopyrroles as Probes of Type 3 Aminoglycoside Kinases

Aminoglycosides are antibiotics that were first identified in the mid 1940’s and have been widely used to treat bacterial infections. These antibiotic agents bind to important cellular components to disrupt bacterial growth and cause cell death. Because of overuse, bacteria have developed methods to destroy the effectiveness of these antibiotics. One common method involves the addition of a chemical group that modifies the antibiotic. To eliminate this particular mode of antibiotic resistance, the chemical modification site must be thoroughly investigated. To this end, groups of diverse compounds must be prepared to obtain data for use in Structure-Activity Relationship (SAR) studies. To obtain these groups, a common structure is identified as a scaffold from which a variety of new compounds can be made quickly, efficiently, and cost effectively. The resultant groups of compounds, or libraries, contain diverse structural components that can be used to systematically investigate the molecular interactions involved within a specific binding site. The synthesis of two series of amidopyrroles are presented.