Discovery and initial development of a novel class of antibacterials: Inhibitors of Staphylococcus aureus transcription/translation

…, MR Hester, JC Ruble, GM Kamilar, DL Romero…

Index: Larsen, Scott D.; Hester, Matthew R.; Craig Ruble; Kamilar, Gregg M.; Romero, Donna L.; Wakefield, Brian; Melchior, Earline P.; Sweeney, Michael T.; Marotti, Keith R. Bioorganic and Medicinal Chemistry Letters, 2006 , vol. 16, # 24 p. 6173 - 6177

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Citation Number: 18

Abstract

The novel bacterial transcription/translation (TT) inhibitor 1 was identified through a combination of high throughput screening and exploratory medicinal chemistry. Initial optimization of the anthranilic acid moiety and sulfonamide amine diversity was accomplished via 1-and two-dimensional solution phase libraries, resulting in an improvement in the MIC of the lead from 64 to 8μg/mL (compound 4l). Subsequent ...