ArticleJournal of enzyme inhibition and medicinal chemistry2019
(Hetero)aryl substituted thiazol-2,4-yl scaffold as human carbonic anhydrase I, II, VII and XIV activators.
Article in Journal of enzyme inhibition and medicinal chemistry, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 8 papers.
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Who cites it
8 citing papers in PubMed, 10 citations in OpenAlex.
- Exploring the Carbonic Anhydrase Activation Properties of 4-arylazo-3,5- diamino-1H-pyrazoles against hCA I, II, IV, and VII isoenzymes.Current topics in medicinal chemistry · 2025Article
- Synthesis, Reaction and Biological Activity of Thiazoles.Current organic synthesis · 2025Review
- Carbonic Anhydrase Activators for Neurodegeneration: An Overview.Molecules (Basel, Switzerland) · 2022Review
- Amine- and Amino Acid-Based Compounds as Carbonic Anhydrase Activators.Molecules (Basel, Switzerland) · 2021Review
- Activation Effects of Carnosine- and Histidine-Containing Dipeptides on Human Carbonic Anhydrases: A Comprehensive Study.International journal of molecular sciences · 2020Article
- The first activation study of the β-carbonic anhydrases from the pathogenic bacteriaJournal of enzyme inhibition and medicinal chemistry · 2019Article
- Activation of human α-carbonic anhydrase isoforms I, II, IV and VII with bis-histamine schiff bases and bis-spinaceamine substituted derivatives.Journal of enzyme inhibition and medicinal chemistry · 2019Article
- Activation Studies of the γ-Carbonic Anhydrases from the Antarctic Marine BacteriaMarine drugs · 2019Article
Corrections and comments
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Authors and funding
5 authors at 3 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Using histamine as lead molecule, a library of (hetero)aryl substituted thiazol-2,4-yl derivatives incorporating pyridine as proton shuttling moiety were obtained and investigated as activators of human carbonic anhydrase (CA, EC 4.2.1.1) isoforms I, II, VII and XIV. Some derivatives displayed good activating and selectivity profiles. This study provides an interesting opportunity to study the thiazole scaffold for the design of CA activators (CAAs), possibly acting on the central nervous system and targeting pathologies involving memory and learning impairments.
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Registered trials
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