Novel small molecule inhibitors targeting the “switch region” of bacterial RNAP: structure-based optimization of a virtual screening hit

…, M Groh, M Negri, J Haupenthal, RW Hartmann

Index: Sahner, J. Henning; Groh, Matthias; Negri, Matthias; Haupenthal, Joerg; Hartmann, Rolf W. European Journal of Medicinal Chemistry, 2013 , vol. 65, p. 223 - 231

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Citation Number: 19

Abstract

Abstract Rising resistance against current antibiotics necessitates the development of antibacterial agents with alternative targets. The “switch region” of RNA polymerase (RNAP), addressed by the myxopyronins, could be such a novel target site. Based on a hit candidate discovered by virtual screening, a small library of 5-phenyl-3-ureidothiophene-2-carboxylic acids was synthesized resulting in compounds with increased RNAP inhibition. Hansch ...