1090932-50-5Relevant academic research and scientific papers
Structure-based ligand design of novel bacterial RNA polymerase inhibitors
McPhillie, Martin J.,Trowbridge, Rachel,Mariner, Katherine R.,O'Neill, Alex J.,Johnson, A. Peter,Chopra, Ian,Fishwick, Colin W. G.
, p. 729 - 734 (2011/11/30)
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.
