ArticleJournal of enzyme inhibition and medicinal chemistry2019
Activation of human α-carbonic anhydrase isoforms I, II, IV and VII with bis-histamine schiff bases and bis-spinaceamine substituted derivatives.
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 15 papers.
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Who cites it
15 citing papers in PubMed, 27 citations in OpenAlex.
- Carbonic anhydrase under the computational lens: a review of advances, challenges, and future directions.Journal of molecular modeling · 2026Review
- 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
- 1,3-Diaryl Triazenes Incorporating Disulfonamides Show Both Antiproliferative Activity and Effective Inhibition of Tumor-associated Carbonic Anhydrases IX and XII.Anti-cancer agents in medicinal chemistry · 2024Article
- Potent carbonic anhydrase I, II, IX and XII inhibition activity of novel primary benzenesulfonamides incorporating bis-ureido moieties.Journal of enzyme inhibition and medicinal chemistry · 2023Article
- Fluconazole-Induced Protein Changes in Osteogenic and Immune Metabolic Pathways of Dental Pulp Mesenchymal Stem Cells of Osteopetrosis Patients.International journal of molecular sciences · 2023Article
- Novel bis-ureido-substituted sulfaguanidines and sulfisoxazoles as carbonic anhydrase and acetylcholinesterase inhibitors.Molecular diversity · 2023Article
- Isocoumarins: a new class of selective carbonic anhydrase IX and XII inhibitors.Journal of enzyme inhibition and medicinal chemistry · 2022Article
- Activation studies with amino acids and amines of a β-carbonic anhydrase fromJournal of enzyme inhibition and medicinal chemistry · 2022Article
- May Sulfonamide Inhibitors of Carbonic Anhydrases fromInternational journal of molecular sciences · 2022Article
- 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 of carbonic anhydrases from human brain by amino alcohol oxime ethers: towards human carbonic anhydrase VII selective activators.Journal of enzyme inhibition and medicinal chemistry · 2021Article
- Reconsidering anion inhibitors in the general context of drug design studies of modulators of activity of the classical enzyme carbonic anhydrase.Journal of enzyme inhibition and medicinal chemistry · 2021Review
- Synthesis of calix[4]azacrown substituted sulphonamides with antioxidant, acetylcholinesterase, butyrylcholinesterase, tyrosinase and carbonic anhydrase inhibitory action.Journal of enzyme inhibition and medicinal chemistry · 2020Article
- Synthesis and carbonic anhydrase activating properties of a series of 2-amino-imidazolines structurally related to clonidineJournal of enzyme inhibition and medicinal chemistry · 2020Article
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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 histamine bis-Schiff bases and bis-spinaceamine derivatives were synthesised and investigated as activators of four human (h) carbonic anhydrase (CA, EC 4.2.1.1) isoforms, the cytosolic hCA I, II and VII, and the membrane-associated hCA IV. All isoforms were effectively activated by the new derivatives, with activation constants in the range of 4.73-10.2 µM for hCA I, 6.15-42.1 µM for hCA II, 2.37-32.7 µM for hCA IV and 32 nM-18.7 µM for hCA VII, respectively. The nature of the spacer between the two histamine/spinaceamine units of these molecules was the main contributor to the diverse activating efficacy, with a very different fine tuning for the diverse isoforms. As CA activators recently emerged as interesting agents for enhancing cognition, in the management of CA deficiencies, or for therapy memory and artificial tissues engineering, our compounds may be considered as candidates for such applications.
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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.