Novel Hybrid-Type Antimicrobial Agents Targeting the Switch Region of Bacterial RNA Polymerase
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- 作者：Fumika Yakushiji ; Yuko Miyamoto ; Yuki Kunoh ; Reiko Okamoto ; Hidemasa Nakaminami ; Yuri Yamazaki ; Norihisa Noguchi ; Yoshio Hayashi
- 刊名：ACS Medicinal Chemistry Letters
- 出版年：2013
- 出版时间：February 14, 2013
- 年：2013
- 卷：4
- 期：2
- 页码：220-224
- 全文大小：351K
- 年卷期：v.4,no.2(February 14, 2013)
- ISSN：1948-5875
文摘
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.