Title |
Discovery of Benzopyrrolizidines as Promising Antigiardiasic Agents
|
---|---|
Published in |
Frontiers in Cellular and Infection Microbiology, January 2022
|
DOI | 10.3389/fcimb.2021.828100 |
Pubmed ID | |
Authors |
Juan Carlos Auriostigue-Bautista, Eduardo Hernández-Vázquez, David González-Calderón, Jorge Luís Figueroa-Romero, Adriana Castillo-Villanueva, Angélica Torres-Arroyo, Martha Ponce-Macotela, Yadira Rufino-González, Mario Martínez-Gordillo, Luis D. Miranda, Jesús Oria-Hernández, Horacio Reyes-Vivas |
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. |
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