RSC Advances

Expanding the scaffold for bacterial RNA polymerase inhibitors: design, synthesis and structure–activity relationships of ureido-heterocyclic-carboxylic acids

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

Index: Elgaher, Walid A. M.; Fruth, Martina; Groh, Matthias; Haupenthal, Joerg; Hartmann, Rolf W. RSC Advances, 2014 , vol. 4, # 5 p. 2177 - 2194

Full Text: HTML

Citation Number: 7

Abstract

The emergence of bacterial resistance requires the development of new antibiotics with an alternative mode of action. Based on class I, developed in our previous study, a new series of RNA polymerase (RNAP) inhibitors targeting the switch region was designed. Feasible synthetic procedures for the aryl-ureido-heterocyclic-carboxylic acids were developed including three regioisomeric thiophene classes (II–IV), as well as three isosteric furan (V, ...