Bromophenols as Candida albicans isocitrate lyase inhibitors

Bioorg Med Chem Lett. 2010 Nov 15;20(22):6644-8. doi: 10.1016/j.bmcl.2010.09.015. Epub 2010 Sep 21.

Abstract

A new series of bromophenols was synthesized by reactions of corresponding phenol analogs with bromine. The synthesized compounds were tested for inhibitory activity against isocitrate lyase (ICL) of Candida albicans and antimicrobial activity against gram-positive and, gram-negative bacteria and fungi. Among the synthesized bromophenols, bis(3-bromo-4,5-dihydroxyphenyl)methanone (11) and (3-bromo-4,5-dihydroxyphenyl)(2,3-dibromo-4,5-dihydroxyphenyl)methanone (12) displayed potent inhibitory activities against ICL, showing a stronger inhibitory effects than were found with natural bromophenol 1. The preliminary structure-activity relationships were investigated in order to determine the essential structural requirements for the inhibitory activities of these compounds against ICL of C. albicans.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anti-Infective Agents / chemistry
  • Anti-Infective Agents / pharmacology*
  • Candida albicans / enzymology*
  • Enzyme Inhibitors / chemistry
  • Enzyme Inhibitors / pharmacology*
  • Isocitrate Lyase / antagonists & inhibitors*
  • Microbial Sensitivity Tests
  • Phenols / pharmacology*
  • Structure-Activity Relationship

Substances

  • Anti-Infective Agents
  • Enzyme Inhibitors
  • Phenols
  • Isocitrate Lyase