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Updated: May 28, 2026
09:04
A Direct, Early Stage Guanidinylation Protocol for the Synthesis of Complex Aminoguanidine-containing Natural Products
Published on: September 9, 2016
Guanidines: Privileged Scaffolds Against Neglected Tropical Diseases: A Review
Luana Ribeiro Dos Anjos1, Rodrigo Santos Aquino de Araújo2, Malu Maria Lucas Dos Reis3
1Fine Organic Chemistry Laboratory School of Sciences and Technology, São Paulo State University (UNESP), Presidente Prudente 19060-080, São Paulo, Brazil.
Pharmaceuticals (Basel, Switzerland)
|May 27, 2026
Summary
Guanidine compounds show promise against neglected parasitic diseases by interacting with vital parasite targets. Further optimization is needed to overcome pharmacokinetic challenges for clinical use.
Area of Science:
- Medicinal Chemistry
- Parasitology
- Drug Discovery
Background:
- Neglected tropical diseases caused by protozoan parasites are a significant global health issue.
- Guanidine derivatives are explored for antiparasitic drug discovery due to their chemical properties and target interactions.
Purpose of the Study:
- To review recent advances in guanidine derivatives for treating neglected parasitic diseases.
- To identify structure-activity relationships and therapeutic potential of guanidine-based compounds.
Main Methods:
- Literature review of studies published in the last decade.
- Analysis of synthetic, natural, and repurposed guanidine-containing compounds.
- Evaluation of antiparasitic activity against various protozoan parasites.
Main Results:
- Guanidine compounds modulate biological activity through electrostatic and hydrogen-bonding interactions with parasite targets.
- Structure-activity relationships indicate the importance of polycationic structures, substituents, and molecular frameworks.
- Compounds show direct antiparasitic effects and potential immunomodulatory properties.
- Pharmacokinetic limitations like poor absorption and permeability hinder clinical translation.
Conclusions:
- Guanidine-based scaffolds offer a promising avenue for developing new therapies against neglected parasitic diseases.
- Further structural optimization is crucial to enhance efficacy, selectivity, and drug-like properties for clinical candidates.
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