Hemozoin Formation as a Target for Antimalarial Drug Design

Abstract

Malaria is the most significant of parasitic diseases accounting for at least one million deaths and over 100 million clinical cases each year in endemic tropical areas of the world. The main thrust of our proposed research is to optimize a tricyclic antimalarial agent for safety and efficacy. Selected tricyclics that have been prepared by us are able to inhibit growth of multidrug resistant strains of Plasmodium falciparum by 50% (IC50) at concentrations well below 1 nanomolar. These same compounds are without cytotoxicity toward human bone marrow progenitors until the concentration is increased more than 10,000-fold. We are currently evaluating these optimized tricyclics in a mouse model of malaria in order to assess toxicity and efficacy.

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Document Details

Document Type
Technical Report
Publication Date
Feb 01, 2005
Accession Number
ADA442977

Entities

People

  • Michael K. Riscoe

Tags

DTIC Thesaurus Topics

  • Anti-Infective Agents
  • Antimalarials
  • Bone Marrow
  • Bones
  • Cells
  • Chemical Synthesis
  • Chemistry
  • Diseases And Disorders
  • Drug Resistance
  • Infectious Diseases
  • Malaria
  • Medical Personnel
  • Parasitic Diseases
  • Resistance
  • Stem Cells
  • Tropical Medicine

Readers

  • Immunology and Pathology
  • Parasitology and Pharmacology of Malaria.
  • Systems Analysis and Design