Antileishmanial activities of 16 synthetic oximino benzocycloalkyl azoles against Leishmania donovani were evaluated in vitro against extracellular promastigotes and intracellular amastigotes. Based on SI (Selectivity Index), five compounds were tested further in vivo in hamster model. Out of these, three compounds have shown medium activity (53-58%) and one has shown significant inhibition of parasite multiplication (70%). Despite the fact that these compounds were better than the existing antileishmanials in respect to IC(50) and SI values, they were less active than miltefosine in vivo. The present study has helped us in identifying a new lead that could be exploited as a potential antileishmanial agent.

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.actatropica.2010.10.011DOI Listing

Publication Analysis

Top Keywords

antileishmanial activity
4
activity benzocycloalkyl
4
benzocycloalkyl azole
4
azole oximino
4
oximino ethers
4
ethers conformationally
4
conformationally constraint
4
constraint analogues
4
analogues oxiconazole
4
oxiconazole antileishmanial
4

Similar Publications

In vitro and in silico approaches manifest the anti-leishmanial activity of wild edible mushroom .

In Silico Pharmacol

December 2024

Laboratory of Cell and Molecular Biology, Department of Botany, Centre of Advanced Study, University of Calcutta, 35 Ballygunge Circular Road, Kolkata, 700019 India.

Visceral Leishmaniasis, caused by is the second most deadly parasitic disease, causing over 65,000 deaths annually. Synthetic drugs available in the market, to combat this disease, have numerous side effects. In this backdrop, we aim to find safer antileishmanial alternatives with minimal side effects from mushrooms, which harbour various secondary metabolites with promising efficacy.

View Article and Find Full Text PDF

Synthesis and in vitro leishmanicidal activity of novel N-arylspermidine derivatives.

Bioorg Chem

December 2024

Universidad de Buenos Aires, CONICET, Cátedra de Química Orgánica II, Departamento de Ciencias Químicas, Facultad de Farmacia y Bioquímica, Junín 956, 1113 Buenos Aires, Argentina. Electronic address:

This work describes the synthesis and biological evaluation of hitherto unknown N-arylspermidine derivatives 3. Compounds 3 were efficiently prepared from cyclic amidines through a novel synthetic approach comprising alkylation with ω-halonitriles followed by reduction. The cyclic N-arylamidine directs the alkylation to the unsubstituted nitrogen and also provides the N-benzyl group present in the triamine after simultaneous reduction of the resulting quaternary salt 2 and the cyano group.

View Article and Find Full Text PDF

Antiparasitic Activity of Coumarin-Chalcone (3-cinnamoyl-2H-chromen-2-ones) Hybrids.

Chem Biodivers

December 2024

Universidad Nacional de Colombia, Antioquia, carrera 65 59a-110, 3840, Medellín, COLOMBIA.

Coumarin-chalcone hybrids are promising compounds that could be used as lead structures in the fight against parasitic diseases. In this work, sixteen hybrids of coumarin-chalcone (3-cinnamoyl-2H-chromen-2-ones) were synthesized, and their in vitro biological activity was evaluated against intracellular amastigotes of Leishmania braziliensis and Trypanosoma cruzi; as well as their cytotoxicity in the U-937 cell line. Compounds (E)-3-(3-(3-ethoxy-4-hydroxyphenyl)acryloyl)-7-methoxy-2H-chromen-2-one (H25) and (E)-7-(diethylamino)-3-(4-(methoxyphenyl)acryloyl)-2H-chromen-2-one (H12) showed the highest antileishmanial activity with EC50 values of 18.

View Article and Find Full Text PDF

Unlabelled: Visceral leishmaniasis (VL), caused by , remains challenging to treat due to severe side effects and increasing drug resistance associated with current chemotherapies. Our study investigates the anti-leishmanial potential of from Uttarakhand, India, with extracts prepared from leaves and stems using ethanol and hexane. Advanced GC-MS analysis identified over 100 bioactive compounds, which were screened using molecular docking to assess their binding to LdHEL-67, a DDX3-DEAD box RNA helicase of donovani.

View Article and Find Full Text PDF

A novel inhibitory strategy of using and killer toxins.

Future Microbiol

December 2024

Department of Biology, Faculty of Biological Sciences, Falavarjan Branch, Islamic Azad University, Isfahan, Iran.

Aim: Leishmaniasis is a globally prevalent parasitic disease that has drawn significant attention. Killer yeasts offer a novel biological control method, presenting a potential alternative for treating leishmaniasis. This study evaluates the antileishmanial activity of and killer toxins against .

View Article and Find Full Text PDF

Want AI Summaries of new PubMed Abstracts delivered to your In-box?

Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!