Novel bis-ureido-substituted sulfaguanidines and sulfisoxazoles as carbonic anhydrase and acetylcholinesterase inhibitors.
Autor: | Lolak N; Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Adıyaman University, 02040, Adiyaman, Turkey. nlolak@adiyaman.edu.tr., Akocak S; Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Adıyaman University, 02040, Adiyaman, Turkey., Durgun M; Department of Chemistry, Faculty of Arts and Sciences, Harran University, 63290, Şanlıurfa, Turkey., Duran HE; Department of Medical Biochemistry, Faculty of Medicine, Kafkas University, 36100, Kars, Turkey., Necip A; Department of Pharmacy Services, Vocational School of Health Services, Harran University, 63300, Şanlıurfa, Turkey., Türkeş C; Department of Biochemistry, Faculty of Pharmacy, Erzincan Binali Yıldırım University, 24002, Erzincan, Turkey. cuneyt.turkes@erzincan.edu.tr., Işık M; Department of Bioengineering, Faculty of Engineering, Bilecik Şeyh Edebali University, 11230, Bilecik, Turkey., Beydemir Ş; Department of Biochemistry, Faculty of Pharmacy, Anadolu University, 26470, Eskişehir, Turkey.; The Rectorate of Bilecik Şeyh Edebali University, 11230, Bilecik, Turkey. |
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Jazyk: | angličtina |
Zdroj: | Molecular diversity [Mol Divers] 2023 Aug; Vol. 27 (4), pp. 1735-1749. Date of Electronic Publication: 2022 Sep 22. |
DOI: | 10.1007/s11030-022-10527-0 |
Abstrakt: | 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 (© 2022. The Author(s), under exclusive licence to Springer Nature Switzerland AG.) |
Databáze: | MEDLINE |
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