Acridine-Based Antimalarials-From the Very First Synthetic Antimalarial to Recent Developments.

Area of Science:

• Medical Parasitology
• Medicinal Chemistry
• Drug Discovery

Background:

• Malaria remains a major global health threat caused by Plasmodium parasites.
• Emerging resistance in Plasmodium falciparum to current antimalarials, including artemisinin combination therapies, necessitates new drug development.
• The repurposing of existing pharmacophores offers a viable strategy to accelerate the discovery of novel antimalarial agents.

Purpose of the Study:

• To review recent advancements in developing safer and more effective antimalarial compounds.
• To highlight the potential of recycling the classical drug quinacrine for novel antimalarial drug design.
• To assess efforts over the past two decades in creating affordable and efficient antimalarial therapies.

Main Methods:

• Literature review of scientific publications and research from the last 20 years.
• Analysis of studies focusing on quinacrine derivatives and their antimalarial activity.
• Evaluation of safety profiles and efficacy of repurposed quinacrine-based compounds.

Main Results:

• Quinacrine, despite historical side effects, exhibits broad biological activity and serves as a promising scaffold.
• Significant progress has been made in modifying quinacrine to enhance efficacy and reduce toxicity.
• Several quinacrine-derived compounds show potent activity against resistant Plasmodium strains.

Conclusions:

• Repurposing quinacrine represents a promising and cost-effective strategy for developing next-generation antimalarial drugs.
• Continued research into quinacrine derivatives is essential to overcome drug resistance and improve malaria treatment.
• The development of safer, affordable, and efficient antimalarial therapies is achievable through scaffold recycling.