Strategically Designed Small Molecules Curb Trophozoite Malaria, Boosting Infected Mice’s Survival

Identifying the Issue

• Spread of multi-drug resistance in the malaria parasite
• Lack of novel therapies and drugs

Objective of the Research

• Development of a novel drug-like candidate with rapid kill kinetics against the malaria parasite Plasmodium falciparum.
• Non-haemolytic and non-toxic to animals.

Who should read this?

Research community working in the Antiplasmodial drug development, medicinal chemists, and pharmaceutical industry.

Solution

Development of nontoxic small molecules with high therapeutic effect and selectivity.

Key Features and Benefits

• Development of small molecules with rapid kill kinetics for plasmodium trophozoite stage
• Non-toxic to mammalian cells and mice
• Non-haemolytic drug-like molecules
• Effective at low micromolar concentrations

Impact

• Oral uptake of the drug for effective therapy
• Minimizing the development of multi-drug resistance in malaria parasites when combined with other therapies
• Effective against drug-resistant parasitic strains

Team

• Hariharan Moorthy, Nitesh Taman, Sai Kiran Mavileti, and Nageswara Rao Golakoti, from the Department of Chemistry, SSSIHL
• Mamta Yadav & Dinkar Sahal, from Malaria Drug Discovery Laboratory, International Centre for Genetic Engineering and Biotechnology (ICGEB), New Delhi
• Labhini Singla & Angshuman Roy Choudhury, Department of Chemical Sciences, from the Indian Institute of Science Education and Research, Mohali

Title of paper: Antiplasmodial and Antimalarial Activity of 3,5-Diarylidenetetrahydro-2H-pyran-4(3H)-ones via Inhibition of Plasmodium falciparum Pyridoxal Synthase

Read Paper Here: https://doi.org/10.1002/cmdc.202200411