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Arch Pharm (Weinheim) ; 357(8): e2300634, 2024 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-38772694

RESUMO

Novel synthesized pyrimidine derivatives were investigated against carbonic anhydrase isoenzymes I and II (hCA I and II), acetylcholinesterase (AChE), butyrylcholinesterase (BChE), α-glycosidase, and aldose reductase (AR) enzymes associated with some common diseases such as epilepsy, glaucoma, Alzheimer's disease, diabetes, and neuropathy. When the results were examined, novel synthesized pyrimidine derivatives were found to have effective inhibition abilities toward the metabolic enzymes. IC50 values and Ki values were calculated for each pyrimidine derivative and compared to positive controls. The synthesized novel pyrimidine derivatives exhibited Ki values in the range of 39.16 ± 7.70-144.62 ± 26.98 nM against hCA I, 18.21 ± 3.66-136.35 ± 21.48 nM toward hCA II, which is associated with different pathological and physiological processes, 33.15 ± 4.85-52.98 ± 19.86 nM on AChE, and 31.96 ± 8.24-69.57 ± 21.27 nM on BChE. Also, Ki values were determined in the range of 17.37 ± 1.11-253.88 ± 39.91 nM against α-glycosidase and 648.82 ± 53.74-1902.58 ± 98.90 nM toward AR enzymes. Within the scope of the study, the inhibition types of the novel synthesized pyrimidine derivatives were evaluated.


Assuntos
Acetilcolinesterase , Butirilcolinesterase , Pirimidinas , Pirimidinas/farmacologia , Pirimidinas/síntese química , Pirimidinas/química , Relação Estrutura-Atividade , Acetilcolinesterase/metabolismo , Butirilcolinesterase/metabolismo , Humanos , Inibidores da Anidrase Carbônica/farmacologia , Inibidores da Anidrase Carbônica/síntese química , Inibidores da Anidrase Carbônica/química , Inibidores da Colinesterase/farmacologia , Inibidores da Colinesterase/síntese química , Inibidores da Colinesterase/química , Estrutura Molecular , Aldeído Redutase/antagonistas & inibidores , Aldeído Redutase/metabolismo , Anidrase Carbônica I/antagonistas & inibidores , Anidrase Carbônica I/metabolismo , Relação Dose-Resposta a Droga , Anidrase Carbônica II/antagonistas & inibidores , Anidrase Carbônica II/metabolismo , Concentração Inibidora 50
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