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  • Title: Novel and potent oxazolidinone antibacterials featuring 3-indolylglyoxamide substituents.
    Author: Takhi M, Singh G, Murugan C, Thaplyyal N, Maitra S, Bhaskarreddy KM, Amarnath PV, Mallik A, Harisudan T, Trivedi RK, Sreenivas K, Selvakumar N, Iqbal J.
    Journal: Bioorg Med Chem Lett; 2008 Sep 15; 18(18):5150-5. PubMed ID: 18768315.
    Abstract:
    Novel oxazolidinone antibacterials bearing a variety of 3-indolylglyoxamide substituents have been explored in an effort to improve the spectrum and potency of this class of agents. A subclass of this series was also made with the diversity at C-5 terminus. These derivatives have been screened against a panel of clinically relevant Gram-positive pathogens and fastidious Gram-negative organisms. Several analogs in this series were identified with in vitro activity superior to linezolid (MIC=0.25-2 microg/mL). Compounds 10a, 10c, 10e and 10f displayed activity against linezolid resistant Gram-positive organisms (MIC=2-4 microg/mL). Selected oxazolidinones were evaluated for in vivo efficacy against a mouse systemic infection model.
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