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.
journal_name
ACS Med Chem Lettjournal_title
ACS medicinal chemistry lettersauthors
McPhillie MJ,Trowbridge R,Mariner KR,O'Neill AJ,Johnson AP,Chopra I,Fishwick CWdoi
10.1021/ml200087msubject
Has Abstractpub_date
2011-07-29 00:00:00pages
729-34issue
10issn
1948-5875journal_volume
2pub_type
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