Ninhydrins inhibit carbonic anhydrases directly binding to the metal ion.
Binding mode
Carbonic anhydrases
Inhibitors
Microwave synthesis
Ninhydrins
Zinc binder
Journal
European journal of medicinal chemistry
ISSN: 1768-3254
Titre abrégé: Eur J Med Chem
Pays: France
ID NLM: 0420510
Informations de publication
Date de publication:
01 Jan 2021
01 Jan 2021
Historique:
received:
30
07
2020
revised:
27
08
2020
accepted:
22
09
2020
pubmed:
16
10
2020
medline:
22
4
2021
entrez:
15
10
2020
Statut:
ppublish
Résumé
Ninhydrins show extensive application in organic chemistry and agriculture whereas they have been poorly investigated as bioactive molecules for medicinal chemistry purposes. A series of ninhydrin derivatives was here investigated for the inhibition of human carbonic anhydrases (CAs, EC 4.2.1.1), based on earlier evidence that gem diols are able to coordinate the metal ion from the CA active site. Ninhydrins demonstrated a micromolar inhibitory action against CA I and IX (K
Identifiants
pubmed: 33059188
pii: S0223-5234(20)30847-3
doi: 10.1016/j.ejmech.2020.112875
pii:
doi:
Substances chimiques
Carbonic Anhydrase Inhibitors
0
Carbonic Anhydrase II
EC 4.2.1.-
Carbonic Anhydrases
EC 4.2.1.1
carbonic anhydrase VI
EC 4.2.1.1
Ninhydrin
HCL6S9K23A
Zinc
J41CSQ7QDS
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
112875Informations de copyright
Copyright © 2020 Elsevier Masson SAS. All rights reserved.
Déclaration de conflit d'intérêts
Declaration of competing interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper.