ArticlePloS one2013
Identification of semicarbazones, thiosemicarbazones and triazine nitriles as inhibitors of Leishmania mexicana cysteine protease CPB.
Article in PloS one, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 19 papers.
What it found
Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.
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.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
19 citing papers in PubMed, 53 citations in OpenAlex.
- Highlights in Cysteine Protease Inhibitors as Antiparasitic Agents Against Trypanosomatids.International journal of molecular sciences · 2026Review
- Multifaceted biological and computational assessment of aromatic and N-heteroaromatic non-substituted thiosemicarbazones.Scientific reports · 2026Article
- IntegratedPharmaceuticals (Basel, Switzerland) · 2026Article
- Target Selectivity of Cysteine Protease Inhibitors: A Strategy to Address Neglected Tropical Diseases.Current medicinal chemistry · 2026Review
- Recent Progress in Thiazole, Thiosemicarbazone, and Semicarbazone Derivatives as Antiparasitic Agents Against Trypanosomatids andMolecules (Basel, Switzerland) · 2025Review
- Advances in Cysteine Protease B Inhibitors for Leishmaniasis Treatment.Current drug targets · 2025Review
- In silico investigation of falcipain-2 inhibition by hybrid benzimidazole-thiosemicarbazone antiplasmodial agents: A molecular docking, molecular dynamics simulation, and kinetics study.Molecular diversity · 2024Article
- Drug Discovery for Cutaneous Leishmaniasis: A Review of Developments in the Past 15 Years.Microorganisms · 2023Review
- ACW-02 an Acridine Triazolidine Derivative Presents Antileishmanial Activity Mediated by DNA Interaction and Immunomodulation.Pharmaceuticals (Basel, Switzerland) · 2023Article
- Discovery of 2-(furan-2-ylmethylene)hydrazine-1-carbothioamide derivatives as novel inhibitors of SARS-CoV-2 main protease.European journal of medicinal chemistry · 2022Article
- Synthesis and Evaluation of Novel 2,2-Dimethylthiochromanones as Anti-Leishmanial Agents.Molecules (Basel, Switzerland) · 2021Article
- Design, synthesis and biological evaluation of N-oxide derivatives with potent in vivo antileishmanial activity.PloS one · 2021Article
- Discovery and Optimization of Triazine Nitrile Inhibitors ofACS chemical neuroscience · 2020Article
- Cysteine proteases in protozoan parasites.PLoS neglected tropical diseases · 2018Review
- Hydrazone Derivatives Enhance Antileishmanial Activity of Thiochroman-4-ones.Molecules (Basel, Switzerland) · 2017Article
- Screening a Natural Product-Based Library against Kinetoplastid Parasites.Molecules (Basel, Switzerland) · 2017Article
- Synthesis and biochemical evaluation of benzoylbenzophenone thiosemicarbazone analogues as potent and selective inhibitors of cathepsin L.Bioorganic & medicinal chemistry · 2015Article
- Trypanothione reductase: a target protein for a combined in vitro and in silico screening approach.PLoS neglected tropical diseases · 2015Article
- Recent developments in drug discovery for leishmaniasis and human African trypanosomiasis.Chemical reviews · 2014Review
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
6 authors at 3 institutions in 2 countries.
Funding
Abstract
Cysteine proteases of the papain superfamily are present in nearly all eukaryotes. They play pivotal roles in the biology of parasites and inhibition of cysteine proteases is emerging as an important strategy to combat parasitic diseases such as sleeping sickness, Chagas' disease and leishmaniasis. Homology modeling of the mature Leishmania mexicana cysteine protease CPB2.8 suggested that it differs significantly from bovine cathepsin B and thus could be a good drug target. High throughput screening of a compound library against this enzyme and bovine cathepsin B in a counter assay identified four novel inhibitors, containing the warhead-types semicarbazone, thiosemicarbazone and triazine nitrile, that can be used as leads for antiparasite drug design. Covalent docking experiments confirmed the SARs of these lead compounds in an effort to understand the structural elements required for specific inhibition of CPB2.8. This study has provided starting points for the design of selective and highly potent inhibitors of L. mexicana cysteine protease CPB that may also have useful efficacy against other important cysteine proteases.
Indexed as
Identifiers
What OpenQuestion holds
Registered trials
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.