The Penn State Research Foundation

Microbiotix, Inc.

Kenneth Charles Keiler

Stephen J Benkovic

Michelle M Butler

Matthew C Torhan

Timothy J Opperman

Jay P Barbor

Steven M Kwasny

Zachary D Aron

John Nandwa Alumasa

Sarah Ellen Ades

Steven C Cardinale

The present invention is related to the development of therapeutics and prophylactics for the treatment and/or prevention of bacterial infections in humans and other mammals. A new class of small molecules is disclosed that inhibits the bacterial trans-translation/ribosome rescue mechanism and thus blocks infection of host cells by bacteria. Also disclosed are methods of using the small molecule inhibitors in the treatment/prevention of bacterial infections.

Metabolically stable N-acylaminooxadiazoles useful as antibacterial agents

Inhibitors of the tmRNA pathway have antibacterial activity with broad species specificity, includingand other pathogens of military and civilian interest. Identified cyclic or linear peptides are further selected by in vivo selection methods, kill bacterial pathogens when added exogenously, and/or eliminate plasmids carrying antibiotic resistance or virulence genes. The molecular target of each cyclic peptide is in the tmRNA pathway and the tmRNA pathway is inhibited in vitro and in vive by the addition of the peptides.

Antibacterial and plasmid elimination agents

Inhibitors of the tmRNA pathway have antibacterial activity with broad species specificity, includingand other pathogens of military and civilian interest. Identified cyclic or linear peptides are further selected by in vivo selection methods, kill bacterial pathogens when added exogenously, and/or eliminate plasmids carrying antibiotic resistance or virulence genes. The molecular target of each cyclic peptide is in the tmRNA pathway and the tmRNA pathway is inhibited in vitro and in vivo by the addition of the peptides.

A compound or its pharmaceutically acceptable salt, as well as a pharmaceutical, composition containing that compound or salt dissolved or dispersed in a pharmaceutically acceptable carrier, and a method of using that compound or salt in an antibacterial treatment. A contemplated compound corresponds in structure to structural Formula I or a pharmaceutically acceptable salt of that compound, wherein V is O or NR, Y is halogen, OR, C-Chydrocarbyl or NHR, Z is NR&#x2014;X&#x2014;Ror CH&#x2014;R, n is 1-6, X is H, S(O), C(O), C(O)NR, C(NH)NRor C(O)O, and R, R, R, R, Rand Rare defined within. 

F2 derivatives as antibacterial agents

A system, a composition, a method and a kit for identifying anti-bacterial agents are provided. The invention described herein is useful in identifying inhibitors of any bacterial stress response. Moreover, the invention can be applied to any sRNA and its target, any transcription factor and its target, and any transcription factor/sRNA pair (i.e., a transcription factor that regulates a sRNA). In particular, the present invention provides a system, a composition, a method and a kit for the identification of cyclic peptides that block the &#x3c3;pathway in

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Boalsburg, PA, United States of America

Kenneth Charles Keiler