Benzimidazole and aminoalcohol derivatives show in vitro anthelmintic activity against Trichuris muris and Heligmosomoides polygyrus
© 2022. The Author(s)..
BACKGROUND: Infections by gastrointestinal nematodes cause significant economic losses and disease in both humans and animals worldwide. The discovery of novel anthelmintic drugs is crucial for maintaining control of these parasitic infections.
METHODS: For this purpose, the aim of the present study was to evaluate the potential anthelmintic activity of three series of compounds against the gastrointestinal nematodes Trichuris muris and Heligmosomoides polygyrus in vitro. The compounds tested were derivatives of benzimidazole, lipidic aminoalcohols and diamines. A primary screening was performed to select those compounds with an ability to inhibit T. muris L1 motility by > 90% at a single concentration of 100 µM; then, their respective IC50 values were calculated. Those compounds with IC50 < 10 µM were also tested against the adult stage of T. muris and H. polygyrus at a single concentration of 10 µM.
RESULTS: Of the 41 initial compounds screened, only compounds AO14, BZ6 and BZ12 had IC50 values < 10 µM on T. muris L1 assay, showing IC50 values of 3.30, 8.89 and 4.17 µM, respectively. However, only two of them displayed activity against the adult stage of the parasites: BZ12 killed 81% of adults of T. muris (IC50 of 8.1 µM) and 53% of H. polygyrus while BZ6 killed 100% of H. polygyrus adults (IC50 of 5.3 µM) but only 17% of T. muris.
CONCLUSIONS: BZ6 and BZ12 could be considered as a starting point for the synthesis of further structurally related compounds.
| Medienart: |
E-Artikel |
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| Erscheinungsjahr: |
2022 |
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| Erschienen: |
2022 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:15 |
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| Enthalten in: |
Parasites & vectors - 15(2022), 1 vom: 08. Juli, Seite 243 |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Valderas-García, Elora [VerfasserIn] |
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| Links: |
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| Themen: |
Aminoalcohol |
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| Anmerkungen: |
Date Completed 12.07.2022 Date Revised 16.07.2022 published: Electronic Citation Status MEDLINE |
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| doi: |
10.1186/s13071-022-05347-y |
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| funding: |
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| Förderinstitution / Projekttitel: |
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NLM343249189 |
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| 245 | 1 | 0 | |a Benzimidazole and aminoalcohol derivatives show in vitro anthelmintic activity against Trichuris muris and Heligmosomoides polygyrus |
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| 500 | |a Date Revised 16.07.2022 | ||
| 500 | |a published: Electronic | ||
| 500 | |a Citation Status MEDLINE | ||
| 520 | |a © 2022. The Author(s). | ||
| 520 | |a BACKGROUND: Infections by gastrointestinal nematodes cause significant economic losses and disease in both humans and animals worldwide. The discovery of novel anthelmintic drugs is crucial for maintaining control of these parasitic infections | ||
| 520 | |a METHODS: For this purpose, the aim of the present study was to evaluate the potential anthelmintic activity of three series of compounds against the gastrointestinal nematodes Trichuris muris and Heligmosomoides polygyrus in vitro. The compounds tested were derivatives of benzimidazole, lipidic aminoalcohols and diamines. A primary screening was performed to select those compounds with an ability to inhibit T. muris L1 motility by > 90% at a single concentration of 100 µM; then, their respective IC50 values were calculated. Those compounds with IC50 < 10 µM were also tested against the adult stage of T. muris and H. polygyrus at a single concentration of 10 µM | ||
| 520 | |a RESULTS: Of the 41 initial compounds screened, only compounds AO14, BZ6 and BZ12 had IC50 values < 10 µM on T. muris L1 assay, showing IC50 values of 3.30, 8.89 and 4.17 µM, respectively. However, only two of them displayed activity against the adult stage of the parasites: BZ12 killed 81% of adults of T. muris (IC50 of 8.1 µM) and 53% of H. polygyrus while BZ6 killed 100% of H. polygyrus adults (IC50 of 5.3 µM) but only 17% of T. muris | ||
| 520 | |a CONCLUSIONS: BZ6 and BZ12 could be considered as a starting point for the synthesis of further structurally related compounds | ||
| 650 | 4 | |a Journal Article | |
| 650 | 4 | |a Aminoalcohol | |
| 650 | 4 | |a Anthelmintic | |
| 650 | 4 | |a Benzimidazole | |
| 650 | 4 | |a Diamine | |
| 650 | 4 | |a Heligmosomoides polygyrus | |
| 650 | 4 | |a Trichuris muris | |
| 650 | 7 | |a Anthelmintics |2 NLM | |
| 650 | 7 | |a Benzimidazoles |2 NLM | |
| 700 | 1 | |a Häberli, Cécile |e verfasserin |4 aut | |
| 700 | 1 | |a Álvarez-Bardón, María |e verfasserin |4 aut | |
| 700 | 1 | |a Escala, Nerea |e verfasserin |4 aut | |
| 700 | 1 | |a Castilla-Gómez de Agüero, Verónica |e verfasserin |4 aut | |
| 700 | 1 | |a de la Vega, Jennifer |e verfasserin |4 aut | |
| 700 | 1 | |a Del Olmo, Esther |e verfasserin |4 aut | |
| 700 | 1 | |a Balaña-Fouce, Rafael |e verfasserin |4 aut | |
| 700 | 1 | |a Keiser, Jennifer |e verfasserin |4 aut | |
| 700 | 1 | |a Martínez-Valladares, María |e verfasserin |4 aut | |
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