Article
Pyrrolamide DNA gyrase inhibitors: fragment-based nuclear magnetic resonance screening to identify antibacterial agents.
Antimicrobial agents and chemotherapy - 1 Mar 2012
Eakin Ann E, Green Oluyinka, Hales Neil, Walkup Grant K, Bist Shanta, Singh Alok, Mullen George, Bryant Joanna, Embrey Kevin, Gao Ning, Breeze Alex, Timms Dave, Andrews Beth, Uria-Nickelsen Maria, Demeritt Julie, Loch James T, Hull Ken, Blodgett April, Illingworth Ruth N, Prince Bryan, Boriack-Sjodin P Ann, Hauck Sheila, MacPherson Lawrence J, Ni Haihong, Sherer Brian
Abstract excerpt
DNA gyrase is an essential enzyme in bacteria, and its inhibition results in the disruption of DNA synthesis and, subsequently, cell death. The pyrrolamides are a novel class of antibacterial agents targeting DNA gyrase. These compounds were identified by a fragment-based lead generation (FBLG) approach using nuclear magnetic resonance (NMR) screening to identify low-molecular-weight compounds that bind to the...
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