ArticleAntimicrobial agents and chemotherapy2016
Novel Heteroaryl Selenocyanates and Diselenides as Potent Antileishmanial Agents.
Article in Antimicrobial agents and chemotherapy, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 18 papers.
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Who cites it
18 citing papers in PubMed.
- Synthesis of novel estradiol bisselenocyanate with unique 2-selenocyano-17-selenocyanoesteryl structure and evaluation of antitumor activity.Molecular diversity · 2025Article
- In vitro and in silico approaches manifest the anti-leishmanial activity of wild edible mushroomIn silico pharmacology · 2025Article
- Promising aryl selenoate derivatives as antileishmanial agents and their effects on gene expression.Antimicrobial agents and chemotherapy · 2024Article
- Evolution of the Quinoline Scaffold for the Treatment of Leishmaniasis: A Structural Perspective.Pharmaceuticals (Basel, Switzerland) · 2024Review
- First-Row Transition 7-Oxo-5-phenyl-1,2,4-triazolo[1,5-a]pyrimidine Metal Complexes: Antiparasitic Activity and Release Studies.Pharmaceuticals (Basel, Switzerland) · 2023Article
- Unveiling a New Selenocyanate as a Multitarget Candidate with Anticancer, Antileishmanial and Antibacterial Potential.Molecules (Basel, Switzerland) · 2022Article
- Evolution of Acridines and Xanthenes as a Core Structure for the Development of Antileishmanial Agents.Pharmaceuticals (Basel, Switzerland) · 2022Review
- Selenium and protozoan parasitic infections: selenocompounds and selenoproteins potential.Parasitology research · 2022Review
- Oral Efficacy of a Diselenide Compound Loaded in Nanostructured Lipid Carriers in a Murine Model of Visceral Leishmaniasis.ACS infectious diseases · 2021Article
- New Phosphoramidates Containing Selenium as Leishmanicidal Agents.Antimicrobial agents and chemotherapy · 2021Article
- Library of Selenocyanate and Diselenide Derivatives as In Vivo Antichagasic Compounds TargetingPharmaceuticals (Basel, Switzerland) · 2021Article
- An On-Demand Dissoluble Chitosan Hydrogel Containing Dynamic Diselenide Bond.Gels (Basel, Switzerland) · 2021Article
- New Amides Containing Selenium as Potent Leishmanicidal Agents Targeting Trypanothione Reductase.Antimicrobial agents and chemotherapy · 2020Article
- Synthesis and Leishmanicidal Activity of Novel Urea, Thiourea, and Selenourea Derivatives of Diselenides.Antimicrobial agents and chemotherapy · 2019Article
- Antileishmanial Evaluation of the Leaf Latex ofEvidence-based complementary and alternative medicine : eCAM · 2019Article
- In vitro screening of known drugs identified by scaffold hopping techniques shows promising leishmanicidal activity for suramin and netilmicin.BMC research notes · 2018Article
- Diglycosyl diselenides alter redox homeostasis and glucose consumption of infective African trypanosomes.International journal for parasitology. Drugs and drug resistance · 2017Article
- Library of Seleno-Compounds as Novel Agents against Leishmania Species.Antimicrobial agents and chemotherapy · 2017Article
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Authors and funding
12 authors.
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Abstract
A series of new selenocyanates and diselenides bearing interesting bioactive scaffolds (quinoline, quinoxaline, acridine, chromene, furane, isosazole, etc.) was synthesized, and their in vitro leishmanicidal activities against Leishmania infantum amastigotes along with their cytotoxicities in human THP-1 cells were determined. Interestingly, most tested compounds were active in the low micromolar range and led us to identify four lead compounds (1h, 2d, 2e, and 2f) with 50% effective dose (ED50) values ranging from 0.45 to 1.27 μM and selectivity indexes of >25 for all of them, much higher than those observed for the reference drugs. These active derivatives were evaluated against infected macrophages, and in order to gain preliminary knowledge about their possible mechanism of action, the inhibition of trypanothione reductase (TryR) was measured. Among these novel structures, compounds 1h (3,5-dimethyl-4-isoxazolyl selenocyanate) and 2d [3,3'-(diselenodiyldimethanediyl)bis(2-bromothiophene)] exhibited good association between TryR inhibitory activity and antileishmanial potency, pointing to 1h, for its excellent theoretical ADME (absorption, distribution, metabolism, and excretion) properties, as the most promising lead molecule for leishmancidal drug design.
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