Novel and potent oxazolidinone antibacterials featuring 3-indolylglyoxamide substituents

Mohamed Takhi, Gurpreet Singh, C. Murugan, Nirvesh Thaplyyal, Soma Maitra, K. M. Bhaskarreddy, P. V.S. Amarnath, Arundhuti Mallik, T. Harisudan, Ravi Kumar Trivedi, K. Sreenivas, N. Selvakumar, Javed Iqbal

Research output: Contribution to journalArticlepeer-review

16 Scopus citations

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 μg/mL). Compounds 10a, 10c, 10e and 10f displayed activity against linezolid resistant Gram-positive organisms (MIC = 2-4 μg/mL). Selected oxazolidinones were evaluated for in vivo efficacy against a mouse systemic infection model.

Original languageEnglish (US)
Pages (from-to)5150-5155
Number of pages6
JournalBioorganic and Medicinal Chemistry Letters
Volume18
Issue number18
DOIs
StatePublished - Sep 15 2008
Externally publishedYes

Keywords

  • Antibacterials
  • Indole
  • Linezolid
  • Oxazolidinones

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