Bioactive peptoids against vector-borne parasitic diseases

Area of Science:

• Medicinal Chemistry
• Parasitology
• Drug Discovery

Background:

• Protozoan parasites cause severe global health issues, including Malaria and Neglected Tropical Diseases (NTDs).
• Existing treatments for these parasitic infections are often ineffective and face emerging drug resistance.
• Novel compound classes are urgently needed for developing new anti-parasitic therapies.

Purpose of the Study:

• To explore the potential of peptoids, a class of peptidomimetics, as novel therapeutic agents against vector-borne parasitic diseases.
• To synthesize and evaluate a diverse library of peptoids for anti-parasitic activity.

Main Methods:

• Preparation of a library of over 50 peptoids with varied chemical functionalities.
• Biological evaluation of the peptoid library against a range of protozoan parasitic targets.
• Determination of IC50 values and selectivity indices (SI) for active compounds.

Main Results:

• Several peptoid compounds demonstrated potent anti-parasitic activity.
• Selected peptoids exhibited good selectivity indices (SI), indicating potential for therapeutic use.
• Peptoid 29 showed significant efficacy against Plasmodium falciparum with an IC50 of 0.05 μM and SI > 100.

Conclusions:

• Peptoids represent a promising class of compounds for developing new treatments against protozoan parasites.
• The findings support further investigation of peptoids for combating Malaria and other NTDs.
• This study highlights the potential of peptoid 29 as a lead compound for anti-parasitic drug development.