Discovery of a New Class of 1-(4-Sulfamoylbenzoyl)piperidine-4-carboxamides as Human Carbonic Anhydrase Inhibitors.
Journal
ACS medicinal chemistry letters
ISSN: 1948-5875
Titre abrégé: ACS Med Chem Lett
Pays: United States
ID NLM: 101521073
Informations de publication
Date de publication:
11 Apr 2024
11 Apr 2024
Historique:
received:
09
11
2023
revised:
16
02
2024
accepted:
22
02
2024
pmc-release:
11
04
2025
medline:
17
4
2024
pubmed:
17
4
2024
entrez:
17
4
2024
Statut:
epublish
Résumé
A series of 1-(4-sulfamoylbenzoyl)piperidine-4-carboxamides deriving from substituted piperazines/benzylamines was designed, synthesized, and tested on human carbonic anhydrase (hCA). The inhibitory activity of the new sulfonamides was analyzed using acetazolamide (AAZ) as a standard inhibitor against hCA I, II, IX, and XII. Several sulfonamides showed both inhibitory activity at low nanomolar concentrations and selectivity against the cytosolic hCA II isoform, and the same trend was observed on the tumor-associated hCA IX and XII. The benzenesulfonamido carboxamides
Identifiants
pubmed: 38628786
doi: 10.1021/acsmedchemlett.3c00484
pmc: PMC11017293
doi:
Types de publication
Journal Article
Langues
eng
Pagination
470-477Informations de copyright
© 2024 American Chemical Society.
Déclaration de conflit d'intérêts
The authors declare no competing financial interest.