Antileishmanial structure-activity relationships of synthetic phospholipids: in vitro and in vivo activities of selected derivatives

Antimicrob Agents Chemother. 2007 Dec;51(12):4525-8. doi: 10.1128/AAC.00465-07. Epub 2007 Oct 1.

Abstract

Antileishmanial activities of 91 synthetic phospholipids against Leishmania donovani were evaluated in vitro and cytotoxicity assessed against two mammalian cell lines. Promising compounds were tested further in vivo. In vitro structure-activity relationships showed a positive contribution of head groups bearing ring systems (N-methylpiperidino and N-methylmorpholino) to antileishmanial activity.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antiprotozoal Agents / chemical synthesis
  • Antiprotozoal Agents / chemistry
  • Antiprotozoal Agents / pharmacology*
  • Cell Line, Tumor
  • Cell Survival / drug effects
  • Cricetinae
  • Humans
  • Inhibitory Concentration 50
  • Leishmania donovani / drug effects*
  • Lethal Dose 50
  • Molecular Structure
  • Phospholipids / chemical synthesis
  • Phospholipids / chemistry
  • Phospholipids / pharmacology*
  • Structure-Activity Relationship*

Substances

  • Antiprotozoal Agents
  • Phospholipids