Pyranocoumarin, a novel anti-TB pharmacophore: synthesis and biological evaluation against Mycobacterium tuberculosis

Bioorg Med Chem. 2006 Jul 1;14(13):4610-26. doi: 10.1016/j.bmc.2006.02.017. Epub 2006 Mar 2.

Abstract

Pyranocoumarin compounds were identified to embody a novel and unique pharmacophore for anti-TB activity. A systematic approach was taken to investigate the structural characteristics. Focused libraries of compounds were synthesized and evaluated for their anti-TB activity in primary screening assays. Compounds shown to be active were further determined for MIC and MBC values. Three of the four bactericidal compounds (16, 17c, and 18f) were amino derivatives, with MIC values of 16 microg/mL and respective MBC values of 32, 32, and 64 microg/mL.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antibiotics, Antitubercular / chemical synthesis
  • Antibiotics, Antitubercular / chemistry*
  • Antibiotics, Antitubercular / pharmacology*
  • Microbial Sensitivity Tests
  • Mycobacterium tuberculosis / drug effects*
  • Pyranocoumarins / chemical synthesis
  • Pyranocoumarins / chemistry*
  • Pyranocoumarins / pharmacology*

Substances

  • Antibiotics, Antitubercular
  • Pyranocoumarins