Synthesis and antifungal activities in vitro of novel pyrazino [2,1-a] isoquinolin derivatives

Bioorg Med Chem Lett. 2010 Feb 1;20(3):979-82. doi: 10.1016/j.bmcl.2009.12.050. Epub 2009 Dec 21.

Abstract

A series of novel pyrazino[2,1-a]isoquinolin compounds were designed and synthesized, and their antifungal activities in vitro were evaluated. The results showed that all of the compounds exhibited antifungal activities. Some of them exhibited stronger antifungal activities than that of lead compounds and among them compound 11b was the most potent one, which showed more potent than that of the active control fluconazole to the four of the five tested fungi. The studies presented here provide a new structural type for the development of novel antifungal agents.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antifungal Agents / chemical synthesis*
  • Antifungal Agents / pharmacology*
  • Aspergillus fumigatus / drug effects
  • Aspergillus fumigatus / physiology
  • Candida albicans / drug effects
  • Candida albicans / physiology
  • Isoquinolines / chemical synthesis*
  • Isoquinolines / pharmacology*
  • Pyrazines / chemical synthesis*
  • Pyrazines / pharmacology*

Substances

  • Antifungal Agents
  • Isoquinolines
  • Pyrazines