Novel bis-ureido-substituted sulfaguanidines and sulfisoxazoles as carbonic anhydrase and acetylcholinesterase inhibitors

Autor: Nebih Lolak, Süleyman Akocak, Mustafa Durgun, Hatice Esra Duran, Adem Necip, Cüneyt Türkeş, Mesut Işık, Şükrü Beydemir
Rok vydání: 2022
Předmět:
Zdroj: Molecular Diversity.
ISSN: 1573-501X
1381-1991
Popis: To discover alternative substances to compounds used to treat many diseases, especially treating Alzheimer's disease (AD) and Parkinson's disease targeting carbonic anhydrase (hCA) and acetylcholinesterase (AChE) enzymes, is important. For this purpose, a series of novel bis-ureido-substituted sulfaguanidine (SG1-4) and sulfisoxazole (SO1-4) derivatives were synthesized, and their inhibitory capacities were screened against hCA isoenzymes (hCA I and II) and AChE. Possible binding mechanisms of inhibitors to the active site were elucidated by in silico studies, and the results were supported by in vitro results. Moreover, the percent radical scavenging capacities of the derivatives were also evaluated. The derivatives (SG1-4 and SO1-4) were more effective against hCAs compared to standard drug acetazolamide (K
Databáze: OpenAIRE
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