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Updated: Apr 28, 2026

In Vitro Transcription Assays and Their Application in Drug Discovery
Published on: September 20, 2016
Structure-based ligand design of novel bacterial RNA polymerase inhibitors
Martin J McPhillie1, Rachel Trowbridge1, Katherine R Mariner1
1School of Chemistry and Faculty of Biological Sciences, University of Leeds , Leeds LS2 9JT, United Kingdom.
Abstract:
Bacterial RNA polymerase (RNAP) is essential for transcription and is an antibacterial target for small molecule inhibitors. The binding region of myxopyronin B (MyxB), a bacterial RNAP inhibitor, offers the possibility of new inhibitor design. The molecular design program SPROUT has been used in conjunction with the X-ray cocrystal structure of Thermus thermophilus RNAP with MyxB to design novel inhibitors based on a substituted pyridyl-benzamide scaffold. A series of molecules, with molecular masses <350 Da, have been prepared using a simple synthetic approach. A number of these compounds inhibited Escherichia coli RNAP.
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