ArticleEuropean journal of medicinal chemistry2012
Synthesis, DNA binding and antileishmanial activity of low molecular weight bis-arylimidamides.
Article in European journal of medicinal chemistry, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 9 papers, 1 of them a synthesis that pooled it.
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Who cites it
9 citing papers in PubMed, 1 synthesis or guideline pooled it.
- Novel amidines and analogues as promising agents against intracellular parasites: a systematic review.Parasitology · 2013Pooled it
- Kinetoplast-Directed Therapies: A Selective Mitochondrial Approach to Combat Leishmaniasis.Pharmaceuticals (Basel, Switzerland) · 2026Review
- Escaping ESKAPE resistance:Royal Society open science · 2023Article
- Synthesis, anti-bacterial and anti-protozoal activities of amidinobenzimidazole derivatives and their interactions with DNA and RNA.Journal of enzyme inhibition and medicinal chemistry · 2018Article
- Evaluation of Transition Metal Complexes of Benzimidazole-Derived Scaffold as Promising Anticancer Chemotherapeutics.Molecules (Basel, Switzerland) · 2018Article
- Antileishmanial Efficacy and Pharmacokinetics of DB766-Azole Combinations.Antimicrobial agents and chemotherapy · 2018Article
- Synthesis and pharmacological evaluation of mono-arylimidamides as antileishmanial agents.Bioorganic & medicinal chemistry letters · 2016Article
- Studies on the antileishmanial mechanism of action of the arylimidamide DB766: azole interactions and role of CYP5122A1.Antimicrobial agents and chemotherapy · 2014Article
- In vitro and in vivo studies of the biological activity of novel arylimidamides against Trypanosoma cruzi.Antimicrobial agents and chemotherapy · 2014Article
Corrections and comments
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Authors and funding
10 authors.
Funding
Abstract
The effects of reducing the molecular weight of the antileishmanial compound DB766 on DNA binding affinity, antileishmanial activity and cytotoxicity are reported. The bis-arylimidamides were prepared by the coupling of aryl S-(2-naphthylmethyl)thioimidates with the corresponding amines. Specifically, we have prepared new series of bis-arylimidamides which include 3a, 3b, 6, 9a, 9b, 9c, 13, and 18. Three compounds 9a, 9c, and 18 bind to DNA with similar or moderately lower affinity to that of DB766, the rest of these compounds either show quite weak binding or no binding at all to DNA. Compounds 9a, 9c, and 13 were the most active against Leishmania amazonensis showing IC(50) values of less than 1 μM, so they were screened against intracellular Leishmania donovani, showing outstanding activity with IC(50) values of 25-79 nM. Despite exhibiting little in vitro cytotoxicity these three compounds were quite toxic to mice.
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Registered trials
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