Discovery of Benzopyrrolizidines as Promising Antigiardiasic Agents
Related Experiment Video
Updated: Oct 5, 2025

Ookluc: A Plasmodium berghei Line for Identifying Transmission-blocking Compounds
Published on: July 11, 2025
Juan Carlos Auriostigue-Bautista1, Eduardo Hernández-Vázquez2, David González-Calderón2
1Laboratorio de Bioquímica-Genética, Instituto Nacional de Pediatría. Insurgentes Sur 3700-C, Col. Insurgentes Cuicuilco, Alcaldía Coyoacán, Ciudad de México, Mexico.
Abstract:
Current treatments for giardiasis include drugs with undesirable side effects, which increase the levels of therapeutic desertion and promote drug resistance in the parasites. Herein, we describe the antigiardiasic evaluation on Giardia lamblia trophozoites of a structurally diverse collection of 74 molecules. Among these scaffolds, we discovered a benzopyrrolizidine derivative with higher antigiardiasic activity (IC50 = 11 µM) and lower cytotoxicity in human cell cultures (IC50 = 130 µM) than those displayed by the current gold-standard drugs (metronidazole and tinidazole). Furthermore, this compound produced morphologic modifications of trophozoites, with occasional loss of one of the nuclei, among other changes not observed with standard giardicidal drugs, suggesting that it might act through a novel mechanism of action.
Related Concept Videos
Aryldiazonium Salts to Azo Dyes: Diazo Coupling
Anxiolytic Drugs: Benzodiazepines and Buspirone
Diazonium Group Substitution with Halogens and Cyanide: Sandmeyer and Schiemann Reactions
Cholinergic Antagonists: Pharmacokinetics
Drugs Affecting GI Tract Motility: Antimicrobials as Antidiarrheal Agents
Drugs Affecting GI Tract Motility: Adsorbents as Antidiarrheal Agents
Adsorbents...

