Design and synthesis of benzenesulfonamide-linked imidazo[2,1-b][1,3,4]thiadiazole derivatives as carbonic anhydrase I and II inhibitors.
Arch Pharm (Weinheim)
; 354(7): e2100028, 2021 Jul.
Article
en En
| MEDLINE
| ID: mdl-33760299
ABSTRACT
A novel series of imidazothiadiazole-linked benzenesulfonamide derivatives (5a-t) was synthesized and subjected for screening against the four physiologically and pharmacologically relevant human carbonic anhydrase (hCA) isoforms hCA I, II, VA, and IX. The compounds selectively inhibited hCA I and II over hCA VA and IX. Furthermore, among the two cytosolic isoforms, hCA II was more effectively inhibited as compared with hCA I. The most active compounds were 5o with K i = 0.246 µM and 5p with K i = 0.376 µM against hCA II, whereas compound 5f showed good inhibition against both hCA I and II with K i = 0.493 and 0.4 µM, respectively. This class of underexplored sulfonamides may be used to design isoform-selective CA inhibitors targeting enzymes of medicinal chemistry interest.
Palabras clave
Texto completo:
1
Banco de datos:
MEDLINE
Asunto principal:
Sulfonamidas
/
Tiadiazoles
/
Imidazoles
Límite:
Humans
Idioma:
En
Año:
2021
Tipo del documento:
Article