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Indole-2-carboxamides Optimization for Antiplasmodial Activity.

Malkeet Kumar1, Anees Ahmad1, Anna Caroline Campos Aguiar2,3

  • 1Institute of Chemistry, University of Campinas, Barão Geraldo, PO Box 6154, Campinas, SP 13083-970, Brazil.

ACS Bio & Med Chem Au
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New antimalarial drug candidates, indole-2-carboxamides, show potent activity against malaria parasites and improved stability. Further research is needed to overcome resistance mechanisms for effective global treatment.

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antimalarialsdrug developmentindolesmalariaresistance

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Area of Science:

  • Medicinal Chemistry
  • Parasitology
  • Drug Discovery

Background:

  • Malaria remains a major global health threat, exacerbated by increasing drug resistance.
  • Novel antimalarial agents with new mechanisms of action are urgently required.

Purpose of the Study:

  • To identify and optimize novel indole-2-carboxamide derivatives as potential antimalarial drugs.
  • To evaluate the potency, metabolic stability, and safety profile of these new compounds.

Main Methods:

  • Synthesis and structural modification of indole-2-carboxamide derivatives.
  • In vitro testing for antimalarial activity (IC50) against Plasmodium falciparum.
  • Assessment of metabolic stability (hMics), hERG channel activity, and hepatic cell cytotoxicity.
  • Mode-of-action studies and cross-resistance evaluation.

Main Results:

  • Optimized compounds (6x) demonstrated potent antimalarial activity (Pf3D7-IC50 ~ 0.3 μM) and good metabolic stability (hMics = 3 μL/min/mg).
  • Compounds exhibited low cardiotoxicity (hERG IC50 > 20 μM) and hepatotoxicity (CC50 > 30 μM).
  • Mechanism involves interference with parasite digestive vacuole homeostasis, but cross-resistance via efflux pumps (PfCRT) was observed.

Conclusions:

  • Indole-2-carboxamides represent a promising scaffold for developing new antimalarial drugs.
  • Further medicinal chemistry efforts are necessary to address cross-resistance and enhance efficacy against resistant strains.