Literature

Abstract

The bacterial RNA polymerase (RNAP) is an ideal target for the development of antimicrobial agents against drug-resistant bacteria. Especially, the switch region within RNAP has been considered as an attractive binding site for drug discovery. Here, we designed and synthesized a series of novel hybrid-type inhibitors of bacterial RNAP. The antimicrobial activities were evaluated using a paper disk diffusion assay, and selected derivatives were tested to determine their MIC values. The hybrid-type antimicrobial agent 29 showed inhibitory activity against Escherichia coli RNAP. The molecular docking study suggested that the RNAP switch region would be the binding site of 29.

DOI： 10.1021/ml300350p

Novel Hybrid-Type Antimicrobial Agents Targeting the Switch Region of Bacterial RNA Polymerase

ACS Medicinal Chemistry Letters 2013.0

Design, synthesis and biological evaluation of novel hybrids of N-aryl pyrrothine-base α-pyrone as bacterial RNA polymerase inhibitors

Bioorganic & Medicinal Chemistry Letters 2020.0

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

European Journal of Medicinal Chemistry 2013.0

Discovery of Novel Bacterial RNA Polymerase Inhibitors: Pharmacophore-Based Virtual Screening and Hit Optimization

Journal of Medicinal Chemistry 2013.0

Structure-Based Ligand Design of Novel Bacterial RNA Polymerase Inhibitors

ACS Medicinal Chemistry Letters 2011.0

Discovery of Antibacterials That Inhibit Bacterial RNA Polymerase Interactions with Sigma Factors