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Updated: Apr 28, 2026

In Vitro Transcription Assays and Their Application in Drug Discovery
Published on: September 20, 2016
Novel hybrid-type antimicrobial agents targeting the switch region of bacterial RNA polymerase
Fumika Yakushiji1, Yuko Miyamoto1, Yuki Kunoh1
1Departments of Medicinal Chemistry and Microbiology, School of Pharmacy, Tokyo University of Pharmacy and Life Sciences , 1432-1 Horinouchi, Hachioji, Tokyo 192-0392, Japan.
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.
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