ArticleJournal of enzyme inhibition and medicinal chemistry2018
Carbonic anhydrases from Trypanosoma cruzi and Leishmania donovani chagasi are inhibited by benzoxaboroles.
Article in Journal of enzyme inhibition and medicinal chemistry, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 27 papers.
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Who cites it
27 citing papers in PubMed, 62 citations in OpenAlex.
- Repositioning FDA-Approved Sulfonamide-Based Drugs as Potential Carbonic Anhydrase Inhibitors inPharmaceuticals (Basel, Switzerland) · 2025Article
- The carbonic anhydrase enzymes as new targets for the management of neglected tropical diseases.Archiv der Pharmazie · 2025Review
- Synthesis and In Vitro Antileishmanial Efficacy of Novel Ethylene Glycol Analogues of Benzothiadiazine-1,1-dioxide.Chemistry & biodiversity · 2025Article
- Advances in the Development of Carbonic Anhydrase Inhibitors as New Antiprotozoal Agents.Current medicinal chemistry · 2024Review
- Targeting Metalloenzymes: The "Achilles' Heel" of Viruses and Parasites.Pharmaceuticals (Basel, Switzerland) · 2023Review
- Thio- and selenosemicarbazones as antiprotozoal agents againstJournal of enzyme inhibition and medicinal chemistry · 2022Article
- Inhibition studies of the protozoan α-carbonic anhydrase fromJournal of enzyme inhibition and medicinal chemistry · 2022Article
- Temporal and Wash-Out Studies Identify Medicines for Malaria Venture Pathogen Box Compounds with Fast-Acting Activity against BothMicroorganisms · 2022Article
- The Boron Advantage: The Evolution and Diversification of Boron's Applications in Medicinal Chemistry.Pharmaceuticals (Basel, Switzerland) · 2022Review
- Activation of the β-carbonic anhydrase from the protozoan pathogenJournal of enzyme inhibition and medicinal chemistry · 2021Article
- Anion inhibition studies of the α-carbonic anhydrases fromJournal of enzyme inhibition and medicinal chemistry · 2021Article
- Organoboron Compounds: Effective Antibacterial and Antiparasitic Agents.Molecules (Basel, Switzerland) · 2021Review
- Synthesis and biological evaluation of new pyrazolebenzene-sulphonamides as potential anticancer agents and hCA I and II inhibitors.Turkish journal of chemistry · 2021Article
- Phosphonamidates are the first phosphorus-based zinc binding motif to show inhibition of β-class carbonic anhydrases from bacteria, fungi, and protozoa.Journal of enzyme inhibition and medicinal chemistry · 2020Article
- A structure-based approach towards the identification of novel antichagasic compounds:Journal of enzyme inhibition and medicinal chemistry · 2020Article
- Benzoxaboroles: New Potent Inhibitors of the Carbonic Anhydrases of the Pathogenic BacteriumACS medicinal chemistry letters · 2020Article
- Article
- Exploring benzoxaborole derivatives as carbonic anhydrase inhibitors: a structural and computational analysis reveals their conformational variability as a tool to increase enzyme selectivity.Journal of enzyme inhibition and medicinal chemistry · 2019Article
- Dual and selective inhibitors of pteridine reductase 1 (PTR1) and dihydrofolate reductase-thymidylate synthase (DHFR-TS) fromJournal of enzyme inhibition and medicinal chemistry · 2019Article
- Appraisal of anti-protozoan activity of nitroaromatic benzenesulfonamides inhibiting carbonic anhydrases fromJournal of enzyme inhibition and medicinal chemistry · 2019Article
Corrections and comments
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Authors and funding
5 authors at 2 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
A series of 6-substituted ureido- and thioureido-benzoxaboroles were investigated as inhibitors of carbonic anhydrases from Trypanosoma cruzi (TcCA), and Leishmania donovani chagasi (LdcCA). Both enzymes were inhibited by benzoxaboroles in the micromolar range. Preferential inhibitory potency against the β-CA LdcCA versus the α-CA TcCA was observed with submicromolar inhibitory activities. Some derivatives displayed excellent inhibitory and selectivity profile over the ubiquitous and physiological relevant human off-target hCA II. This study provides a convincing opportunity to study benzoxaborole scaffold for the design of antiprotozoan potential drugs targeting the pathogen's carbonic anhydrases.
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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.