ArticleAntimicrobial agents and chemotherapy2015
Leishmanicidal activities of novel methylseleno-imidocarbamates.
Article in Antimicrobial agents and chemotherapy, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 21 papers.
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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Who cites it
21 citing papers in PubMed, 30 citations in OpenAlex.
- Leishmanicidal Action of the Peptides 19-4LF, 19-2.5 and 19-2.5LF Topically Administered on Cutaneous Lesions Caused byPharmaceutics · 2026Article
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- Promising aryl selenoate derivatives as antileishmanial agents and their effects on gene expression.Antimicrobial agents and chemotherapy · 2024Article
- Repurposing the Antibacterial Agents Peptide 19-4LF and Peptide 19-2.5 for Treatment of Cutaneous Leishmaniasis.Pharmaceutics · 2022Article
- The BRCT Domain from the Homologue of the Oncogene PES1 inInternational journal of molecular sciences · 2022Article
- Selenium and protozoan parasitic infections: selenocompounds and selenoproteins potential.Parasitology research · 2022Review
- InInternational journal of molecular sciences · 2021Article
- Discovery and Validation of Lmj_04_BRCT Domain, a Novel Therapeutic Target: Identification of Candidate Drugs for Leishmaniasis.International journal of molecular sciences · 2021Article
- New Phosphoramidates Containing Selenium as Leishmanicidal Agents.Antimicrobial agents and chemotherapy · 2021Article
- Activity of Anti-Microbial Peptides (AMPs) againstBiomolecules · 2021Review
- Potential therapeutic targets shared between leishmaniasis and cancer.Parasitology · 2021Review
- New Amides Containing Selenium as Potent Leishmanicidal Agents Targeting Trypanothione Reductase.Antimicrobial agents and chemotherapy · 2020Article
- LmjF.22.0810 fromBiomedicines · 2020Article
- The Novel Serine/Threonine Protein Kinase LmjF.22.0810 fromBiomolecules · 2019Article
- Synthesis and Leishmanicidal Activity of Novel Urea, Thiourea, and Selenourea Derivatives of Diselenides.Antimicrobial agents and chemotherapy · 2019Article
- Selenocompounds as Novel Antibacterial Agents and Bacterial Efflux Pump Inhibitors.Molecules (Basel, Switzerland) · 2019Article
- Leishmanicidal Activity of Isoselenocyanate Derivatives.Antimicrobial agents and chemotherapy · 2019Article
- In vitro screening of known drugs identified by scaffold hopping techniques shows promising leishmanicidal activity for suramin and netilmicin.BMC research notes · 2018Article
- Library of Seleno-Compounds as Novel Agents against Leishmania Species.Antimicrobial agents and chemotherapy · 2017Article
- Construction of Two mCherry Plasmids (pXG-mCherry) for TransgenicJournal of parasitology research · 2017Article
Corrections and comments
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Authors and funding
11 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The generation of new antileishmanial drugs has become a priority. Selenium and its derivatives stand out as having promising leishmanicidal activity. In fact, some parasites express selenoproteins and metabolize selenium. Recently, selenium derivatives have shown the potential to reduce parasitemia, clinical manifestations, and mortality in parasite-infected mice. In this paper, after selecting four candidates according to drug similarity parameters, we observed that two of them, called compounds 2b [methyl-N,N'-di(thien-2-ylcarbonyl)-imidoselenocarbamate] and 4b [methyl-N,N'-di(5-nitrothien-3-ylcarbonyl)-imidoselenocarbamate], exhibit low 50% inhibitory concentrations (IC50s) (<3 μM) and good selectivity indexes (SIs) (>5) in Leishmania major promastigotes and lack toxicity on macrophages. In addition, in analysis of their therapeutic potential against L. major in vitro infection, both compounds display a dramatic reduction of amastigote burden (∼80%) with sublethal concentrations. Furthermore, in macrophages, these selenocompounds induce nitric oxide production, which has been described to be critical for defense against intracellular pathogens. Compounds 2b and 4b were demonstrated to cause cell cycle arrest in G1. Interestingly, evaluation of expression of genes related to proliferation (PCNA), treatment resistance (ABC transporter and alpha-tubulin), and virulence (quinonoid dihydropteridine reductase [QDPR]) showed several alterations in gene expression profiling. All these results prompt us to propose both compounds as candidates to treat leishmanial infections.
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.