التفاصيل البيبلوغرافية
| العنوان: |
Discovery of Benzopyrrolizidines as Promising Antigiardiasic Agents |
| المؤلفون: |
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 |
| المصدر: |
Frontiers in Cellular and Infection Microbiology, Vol 11 (2022) |
| بيانات النشر: |
Frontiers Media S.A., 2022. |
| سنة النشر: |
2022 |
| المجموعة: |
LCC:Microbiology |
| مصطلحات موضوعية: |
Giardia, antigiardiasic, benzopyrrolizidine, chemical library, drug design, chemotherapy, Microbiology, QR1-502 |
| الوصف: |
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. |
| نوع الوثيقة: |
article |
| وصف الملف: |
electronic resource |
| اللغة: |
English |
| تدمد: |
2235-2988 |
| Relation: |
https://www.frontiersin.org/articles/10.3389/fcimb.2021.828100/full; https://doaj.org/toc/2235-2988 |
| DOI: |
10.3389/fcimb.2021.828100 |
| URL الوصول: |
https://doaj.org/article/9461f2496c6c4732813761cab442627e |
| رقم الانضمام: |
edsdoj.9461f2496c6c4732813761cab442627e |
| قاعدة البيانات: |
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