Leishmanicidal activity of aliphatic and aromatic lactones: correlation structure-activity

Molecules. 2009 Jul 10;14(7):2491-500. doi: 10.3390/molecules14072491.

Abstract

Several aliphatic and aromatic lactones and two dimers were synthesized using the sequence: allylation - esterification - metathesis. These compounds were active in vitro against intracellular amastigotes of Leishmania panamensis. The structure-activity relationship showed the importance of the aliphatic side chain to enhance the biological activity and to obtain lower cytotoxicity. It was also observed that a decrease in the size of the lactone ring increases the selectivity index.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antiprotozoal Agents / chemical synthesis
  • Antiprotozoal Agents / chemistry*
  • Antiprotozoal Agents / pharmacology
  • Lactones / chemical synthesis
  • Lactones / chemistry*
  • Lactones / pharmacology
  • Leishmania guyanensis / drug effects*
  • Structure-Activity Relationship

Substances

  • Antiprotozoal Agents
  • Lactones