NOC chemistry for tuberculosis - Further investigations on the structure-activity relationships of antitubercular isoxazole-3-carboxylic acid ester derivatives

Marco Pieroni, Annamaria Lilienkampf, Yuehong Wang, Baojie Wan, Sanghyun Cho, Scott G. Franzblau, Alan P. Kozikowski

Research output: Contribution to journalArticlepeer-review

Abstract

NOC, NOC! Who's there? We have expanded the body of structure-activity relationships (SAR) regarding the 3-isoxazolecarboxylic acid ethyl esters by the design and synthesis of 5-aryl- and 5-[(N-aryl)amino]methyl analogues. Compounds were active against Mycobacterium tuberculosis (Mtb) at sub-micromolar concentrations and, for selected compounds, no toxicity was observed on Vero cells.

Original languageEnglish (US)
Pages (from-to)1667-1672
Number of pages6
JournalChemMedChem
Volume5
Issue number10
DOIs
StatePublished - Oct 4 2010

Keywords

  • Drug design
  • Drug discovery
  • Isoxazole derivatives
  • Tuberculosis

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Pharmacology
  • Drug Discovery
  • Pharmacology, Toxicology and Pharmaceutics(all)
  • Organic Chemistry

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