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Pulvinones as bacterial cell wall biosynthesis inhibitors |
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| Authors: | Antane Schuyler Caufield Craig E Hu William Keeney David Labthavikul Pornpen Morris Koi Naughton Shaughnessy M Petersen Peter J Rasmussen Beth A Singh Guy Yang Youjun |
| Institution: | Medicinal Chemistry, Chemical and Screening Sciences, Wyeth Research, Princeton, NJ 08543, USA. antanes@wyeth.com |
| Abstract: | Pulvinones were synthesized (>180) in arrays and evaluated as inhibitors of early stage cell wall biosynthesis enzymes MurA-MurD. Several pulvinones inhibited Mur enzymes with IC(50)'s in the 1-10 microg/mL range and demonstrated antibacterial activity against Gram-positive bacteria including methicillin-resistant Staphyloccus aureus, vancomycin-resistant Enterococcus faecalis, and penicillin-resistant Streptococcus pneumoniae. |
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