Mechanisms of Action of Substituted β-Amino Alkanols on Leishmania donovani

Abengózar, María Ángeles; Bustos, Luis A.; García-Hernández, Raquel; Palencia, Pilar Fernández de; Escarcena, Ricardo; Castanys, Santiago; Olmo, Esther del; Gamarro, Francisco; Feliciano, Arturo San; Rivas, Luís

doi:10.1128/aac.04003-14

Cited by 5 publications

(3 citation statements)

References 55 publications

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“…Moreover, some novel heteroretinoidbisbenzylidine ketone hybrids have been synthesized and evaluated by Tiwari et al [51] for their in vitro activity against L. donovani; a new class of compounds with antileishmanial activity was identified. Also, N-substituted β-amino alkanols were recently shown to have leishmanicidal activity, inducing severe mitochondrial swelling and vesiculation of the parasite [52].…”

Section: Treatmentmentioning

confidence: 99%

Recent updates and perspectives on leishmaniasis

Savoia

2015

J Infect Dev Ctries

143

127

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Leishmaniasis is a neglected vector-borne tropical infection considered to be a disease of the poor. Concentrated in poverty-stricken countries within Southeast Asia, East Africa, and Latin America, it is also endemic in several Mediterranean countries. The management of the heterogeneous syndromes determined by parasites belonging to the genus Leishmania is particularly difficult in developed, non-endemic countries owing to the unfamiliarity of physicians with clinical symptoms, diagnostic possibilities, and available treatment options. Therefore, travelers and other people who may be exposed to sand flies in endemic areas should receive counseling regarding leishmaniasis and appropriate protective measures. Serological diagnosis is rarely used for cutaneous and mucocutaneous diseases, but it is the most commonly used technique for visceral leishmaniasis. The drugs used to treat this last disease are expensive and sometimes have toxic side effects. This review highlights the diagnostic, chemotherapeutic, and immunizing strategies to control leishmaniasis, though no human vaccine is commercially available currently owing to the complexity of the cellular immune response to this parasite.

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Section: Treatmentmentioning

confidence: 99%

Recent updates and perspectives on leishmaniasis

Savoia

2015

J Infect Dev Ctries

143

127

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“…The anthelmintic activity of most of these compounds was previously tested in vitro against the gastrointestinal nematode infecting sheep Teladorsagia circumcincta [ 18 , 21 ] and some of them were also tested against Leishmania spp. [ 31 , 32 ], Trypanosoma spp. [ 17 , 33 ] and Strongyloides venezuelensis [ 34 ].…”

Section: Discussionmentioning

confidence: 99%

Benzimidazole and aminoalcohol derivatives show in vitro anthelmintic activity against Trichuris muris and Heligmosomoides polygyrus

et al. 2022

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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. Graphical Abstract

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“…The anthelmintic activity of most of these compounds were previously tested in vitro against the gastrointestinal nematode infecting sheep Teladorsagia circumcincta [18,21] and some of them were also tested against Leishmania sp. [31,32], Trypanosoma sp. [17,33] and Strongyloides venezuelensis [34].…”

Section: Discussionmentioning

confidence: 99%

Benzimidazole and aminoalcohol derivatives show in vitro anthelmintic activity against Trichuris muris and Heligmosomoides polygyrus

Valladares

Valderas-García

Häberli

et al. 2022

Preprint

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Background: Infections by gastrointestinal nematodes cause significant economic losses and disease in both human 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 more than 90% at a single concentration of 100 µM, and then, their respective IC50 values were calculated. Those compounds with IC50 lower than 10 µM were also tested against the adult stage of T. muris and H. polygyrus at a single concentration of 10µM. Results: Of the 41 initial compounds screened, only compounds AO14, BZ6 and BZ12 had IC50 values lower than 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 potential candidates for further in vivo efficacy testing.

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Mechanisms of Action of Substituted β-Amino Alkanols on Leishmania donovani

Cited by 5 publications

References 55 publications

Recent updates and perspectives on leishmaniasis

Recent updates and perspectives on leishmaniasis

Benzimidazole and aminoalcohol derivatives show in vitro anthelmintic activity against Trichuris muris and Heligmosomoides polygyrus

Benzimidazole and aminoalcohol derivatives show in vitro anthelmintic activity against Trichuris muris and Heligmosomoides polygyrus

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