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Bioactive peptoids against vector-borne parasitic diseases.

Hannah L Bolt1, Marcel Kaiser2, Yu Luo3

  • 1Department of Chemistry, Durham University, South Road, Durham DH1 3LE, UK.

Bioorganic & Medicinal Chemistry Letters
|November 1, 2025
PubMed
Summary

New peptoids show potent activity against protozoan parasites like Malaria, offering hope against drug resistance. This research explores novel treatments for neglected tropical diseases (NTDs) and vector-borne illnesses.

Keywords:
AntiparasiticMalariaNTDsNeglected tropical diseasesParasitesPeptoids

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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.