Synthesis and anti-Candida activity of novel 2-hydrazino-1,3-thiazole derivatives

Bioorg Med Chem Lett. 2013 Mar 15;23(6):1803-7. doi: 10.1016/j.bmcl.2013.01.039. Epub 2013 Jan 23.

Abstract

Eighteen new hydrazino-1,3-thiazole derivatives were evaluated against 8 strains of multi-resistant Candida spp. Introduction of an indolyl moiety linked to the hydrazone function enhanced the in vitro anti-Candida activity, with an activity spectrum towards Candida albicans strains. Introduction of a (S)-2-aminoethyl chain on the thiazole nucleus largely enhanced the in vitro antifungal activity, with a selectivity oriented towards non-C. albicans species.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antifungal Agents / chemical synthesis*
  • Antifungal Agents / pharmacology
  • Antifungal Agents / toxicity
  • Candida / drug effects
  • Candida albicans / drug effects
  • Cell Survival / drug effects
  • Drug Resistance, Fungal / drug effects
  • Mice
  • Microbial Sensitivity Tests
  • NIH 3T3 Cells
  • Structure-Activity Relationship
  • Thiazoles / chemistry*
  • Thiazoles / pharmacology
  • Thiazoles / toxicity

Substances

  • Antifungal Agents
  • Thiazoles