Evaluation of (4-aminobutyloxy)quinolines as a novel class of antifungal agents

Bioorg Med Chem Lett. 2013 Aug 15;23(16):4641-3. doi: 10.1016/j.bmcl.2013.06.014. Epub 2013 Jun 13.

Abstract

Antifungal assessment of eighteen 5-, 6- and 8-(4-aminobutyloxy)quinolines revealed a significant susceptibility of the tested fungi and yeast strains (Candida albicans, Rhodotorula bogoriensis, Aspergillus flavus and Fusarium solani) toward different halo-substituted 8-(4-aminobutyloxy)quinolines. The six most potent compounds displayed antifungal activities similar to those of established antifungal agents such as Amphotericin B, Fluconazole and Itraconazole, and one representative also showed a promising broad-spectrum antifungal profile. The introduction of an aminoalkoxy side chain at the 8-position of a halo-substituted quinoline core might thus provide a new class of lead structures in the search for novel antifungal agents.

Keywords: Antifungal agents; Mycoses; Quinolines.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amines / chemical synthesis
  • Amines / chemistry
  • Amines / pharmacology
  • Amphotericin B / chemistry
  • Amphotericin B / pharmacology
  • Antifungal Agents / chemical synthesis
  • Antifungal Agents / chemistry
  • Antifungal Agents / pharmacology*
  • Candida albicans / drug effects*
  • Microbial Sensitivity Tests
  • Molecular Structure
  • Quinolines / chemical synthesis
  • Quinolines / chemistry
  • Quinolines / pharmacology*

Substances

  • Amines
  • Antifungal Agents
  • Quinolines
  • Amphotericin B