New isoxazolidinyl-based N-alkylethanolamines as new activators of human brain carbonic anhydrases.

ABSTRACT: Carbonic anhydrases (CAs) are widespread metalloenzymes which catalyse the reversible hydration of carbon dioxide (CO₂) to bicarbonate (HCO₃^-) and a proton, relevant in many physiological processes. In the last few years, the involvement of CA activation in different metabolic pathways in the human brain addressed the research to the discovery of novel CA activators. Here, a new series of isoxazoline-based amino alcohols as CA activators was investigated. The synthesis and the CA activating effects towards four human CA isoforms expressed in the human brain, that are hCAs I, II, IV and VII, were reported. The best results were obtained for the (methyl)-isoxazoline-amino alcohols 3 and 5 with K_A values in the submicromolar range (0.5

SUBMITTER: Cuffaro D 

PROVIDER: S-EPMC9848372 | biostudies-literature | 2023 Dec

REPOSITORIES: biostudies-literature