The antibiotic furagin and its derivatives are isoform-selective human carbonic anhydrase inhibitors.

Anti-Bacterial Agents / chemical synthesis Carbonic Anhydrase Inhibitors / chemical synthesis Carbonic Anhydrases / metabolism Crystallography, X-Ray Dose-Response Relationship, Drug Furagin / analogs & derivatives Humans Hydrophobic and Hydrophilic Interactions Isoenzymes / antagonists & inhibitors Models, Molecular Molecular Structure Structure-Activity Relationship
Carbonic anhydrase inhibitors furagin hydantoin molecular dynamics synthesis

Journal

Journal of enzyme inhibition and medicinal chemistry
ISSN: 1475-6374
Titre abrégé: J Enzyme Inhib Med Chem
Pays: England
ID NLM: 101150203

Informations de publication

Date de publication:
Dec 2020
Historique:
entrez: 17 4 2020
pubmed: 17 4 2020
medline: 22 12 2020
Statut: ppublish

Résumé

The clinically used antibiotic Furagin and its derivatives possess inhibitory activity on human (h) carbonic anhydrases (CA, EC 4.2.1.1), some of which are highly expressed in various tissues and malignancies (hCA IX/XII). Furagin exhibited good hCA IX and XII inhibition with

Identifiants

DOI: 10.1080/14756366.2020.1752201 PMID: 32297543 PMC: PMC7178874
pubmed: 32297543
doi: 10.1080/14756366.2020.1752201
pmc: PMC7178874
doi:

Substances chimiques

Anti-Bacterial Agents 0
Carbonic Anhydrase Inhibitors 0
Isoenzymes 0
Carbonic Anhydrases EC 4.2.1.1
Furagin K2R4N34Y9I

Types de publication

Journal Article

Langues

eng

Sous-ensembles de citation

IM

Pagination

1011-1020

Références

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Auteurs

Aleksandrs Pustenko (A)

Latvian Institute of Organic Synthesis, Riga, Latvia.
Institute of Technology of Organic Chemistry, Faculty of Materials Science and Applied Chemistry, Riga Technical University, Riga, Latvia.

Alessio Nocentini (A)

Department of NEUROFARBA, Section of Pharmaceutical and Nutraceutical Sciences, University of Florence, Firenze, Italy.
Department of NEUROFARBA, Section of Pharmaceutical and Nutraceutical Sciences, Laboratory of Molecular Modeling Cheminformatics & QSAR, University of Florence, Firenze, Italy.

Paola Gratteri (P)

Department of NEUROFARBA, Section of Pharmaceutical and Nutraceutical Sciences, Laboratory of Molecular Modeling Cheminformatics & QSAR, University of Florence, Firenze, Italy.

Alessandro Bonardi (A)

Department of NEUROFARBA, Section of Pharmaceutical and Nutraceutical Sciences, University of Florence, Firenze, Italy.
Department of NEUROFARBA, Section of Pharmaceutical and Nutraceutical Sciences, Laboratory of Molecular Modeling Cheminformatics & QSAR, University of Florence, Firenze, Italy.

Igor Vozny (I)

Latvian Institute of Organic Synthesis, Riga, Latvia.

Raivis Žalubovskis (R)

Latvian Institute of Organic Synthesis, Riga, Latvia.
Institute of Technology of Organic Chemistry, Faculty of Materials Science and Applied Chemistry, Riga Technical University, Riga, Latvia.

Claudiu T Supuran (CT)

Department of NEUROFARBA, Section of Pharmaceutical and Nutraceutical Sciences, University of Florence, Firenze, Italy.
ORCID: 0000-0003-4262-0323

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Classifications MeSH

questionsmedicales.fr › Actions chimiques et utilisations › Actions pharmacologiques › Utilisations thérapeutiques › Anti-infectieux › Antibactériens › The antibiotic furagin and its derivatives are...
questionsmedicales.fr › Actions chimiques et utilisations › Actions pharmacologiques › Mécanismes moléculaires de l'action pharmacologique › Antienzymes › Inhibiteurs de l'anhydrase carbonique › The antibiotic furagin and its derivatives are...
questionsmedicales.fr › Enzymes et coenzymes › Enzymes › Lyases › Carbon-oxygen lyases › Hydro-lyases › Carbonic anhydrases › The antibiotic furagin and its derivatives are...
questionsmedicales.fr › Techniques d'investigation › Techniques de chimie analytique › Cristallographie aux rayons X › The antibiotic furagin and its derivatives are...
questionsmedicales.fr › Phénomènes physiologiques › Phénomènes pharmacologiques et toxicologiques › Phénomènes toxicologiques › Relation dose-effet des médicaments › The antibiotic furagin and its derivatives are...
questionsmedicales.fr › Composés hétérocycliques › Composés hétéromonocycliques › Furanes › Nitrofuranes › Furagine › The antibiotic furagin and its derivatives are...
questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Primates › Haplorhini › Catarrhini › Hominidae › Humains › The antibiotic furagin and its derivatives are...
questionsmedicales.fr › Phénomènes chimiques › Interactions hydrophobes et hydrophiles › The antibiotic furagin and its derivatives are...
questionsmedicales.fr › Acides aminés, peptides et protéines › Protéines › Isoformes de protéines › Isoenzymes › The antibiotic furagin and its derivatives are...
questionsmedicales.fr › Techniques d'investigation › Modèles théoriques › Modèles moléculaires › The antibiotic furagin and its derivatives are...
questionsmedicales.fr › Phénomènes chimiques › Structure moléculaire › The antibiotic furagin and its derivatives are...
questionsmedicales.fr › Phénomènes physiologiques › Phénomènes pharmacologiques et toxicologiques › Phénomènes pharmacologiques › Relation structure-activité › The antibiotic furagin and its derivatives are...