ArticleJournal of enzyme inhibition and medicinal chemistry2017
Synthesis and biological evaluation of histamine Schiff bases as carbonic anhydrase I, II, IV, VII, and IX activators.
Article in Journal of enzyme inhibition and medicinal chemistry, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 25 papers.
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Who cites it
25 citing papers in PubMed, 64 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
- 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
- New Ni(II) and Pd(II) complexes bearing derived sulfa drug ligands: synthesis, characterization, DFT calculations, and in silico and in vitro biological activity studies.Biometals : an international journal on the role of metal ions in biology, biochemistry, and medicine · 2023Article
- Synthesis and Molecular Docking of New N-Acyl Hydrazones- Benzimidazole as hCA I and II Inhibitors.Medicinal chemistry (Shariqah (United Arab Emirates)) · 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
- Carbonic Anhydrase Activators for Neurodegeneration: An Overview.Molecules (Basel, Switzerland) · 2022Review
- New Histamine-Related Five-Membered N-Heterocycle Derivatives as Carbonic Anhydrase I Activators.Molecules (Basel, Switzerland) · 2022Article
- Amine- and Amino Acid-Based Compounds as Carbonic Anhydrase Activators.Molecules (Basel, Switzerland) · 2021Review
- Activation studies of the β-carbonic anhydrases fromJournal 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
- Synthesis and carbonic anhydrase activating properties of a series of 2-amino-imidazolines structurally related to clonidineJournal of enzyme inhibition and medicinal chemistry · 2020Article
- 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
- (Hetero)aryl substituted thiazol-2,4-yl scaffold as human carbonic anhydrase I, II, VII and XIV activators.Journal of enzyme inhibition and medicinal chemistry · 2019Article
- Synthesis and biological evaluation of novel 3-(quinolin-4-ylamino)benzenesulfonamidesAQ3 as carbonic anhydrase isoforms I and II inhibitors.Journal of enzyme inhibition and medicinal chemistry · 2019Article
- 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
- Synthesis and biological evaluation of novel 8-substituted quinoline-2-carboxamides as carbonic anhydrase inhibitors.Journal of enzyme inhibition and medicinal chemistry · 2019Article
- Investigation of piperazines as human carbonic anhydrase I, II, IV and VII activators.Journal of enzyme inhibition and medicinal chemistry · 2018Article
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
A series of 20 histamine Schiff base was synthesised by reaction of histamine, a well known carbonic anhydrase (CA, E.C 4.2.2.1.) activator pharmacophore, with substituted aldehydes. The obtained histamine Schiff bases were assayed as activators of five selected human (h) CA isozymes, the cytosolic hCA I, hCA II, and hCA VII, the membrane-anchored hCA IV and transmembrane hCA IX. Some of these compounds showed efficient activity (in the nanomolar range) against the cytosolic isoform hCA VII, which is a key CA enzyme involved in brain metabolism. Moderate activity was observed against hCA I and hCA IV (in the nanomolar to low micromolar range). The structure-activity relationship for activation of these isoforms with the new histamine Schiff bases is discussed in detail based on the nature of the aliphatic, aromatic, or heterocyclic moiety present in the aldehyde fragment of the molecule, which may participate in diverse interactions with amino acid residues at the entrance of the active site, where activators bind, and which is the most variable part among the different CA isoforms.
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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.