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  • Title: Pyrrolamide DNA gyrase inhibitors: optimization of antibacterial activity and efficacy.
    Author: Sherer BA, Hull K, Green O, Basarab G, Hauck S, Hill P, Loch JT, Mullen G, Bist S, Bryant J, Boriack-Sjodin A, Read J, DeGrace N, Uria-Nickelsen M, Illingworth RN, Eakin AE.
    Journal: Bioorg Med Chem Lett; 2011 Dec 15; 21(24):7416-20. PubMed ID: 22041057.
    Abstract:
    The pyrrolamides are a new class of antibacterial agents targeting DNA gyrase, an essential enzyme across bacterial species and inhibition results in the disruption of DNA synthesis and subsequently, cell death. The optimization of biochemical activity and other drug-like properties through substitutions to the pyrrole, piperidine, and heterocycle portions of the molecule resulted in pyrrolamides with improved cellular activity and in vivo efficacy.
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