Vinyl functionalized 5,6-dimethylbenzimidazolium salts: Synthesis and biological activities
Küçük Resim Yok
Tarih
2023
Dergi Başlığı
Dergi ISSN
Cilt Başlığı
Yayıncı
Wiley
Erişim Hakkı
info:eu-repo/semantics/closedAccess
Özet
A series of vinyl functionalized 5,6-dimethylbenzimidazolium salts are synthesized. All compounds were fully characterized by elemental analyses, MS, H-1-NMR, C-13-NMR, and IR spectroscopy techniques. Enzyme inhibition is a very active area of research in drug design and development. In this study, the synthesized novel benzimidazolium salts were evaluated toward the human erythrocyte carbonic anhydrase I (hCA I), and II (hCA II) isoenzymes, acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) enzymes. They demonstrated highly potent inhibition ability against hCA I with K-i values of 484.8 +/- 62.6-1389.7 +/- 243.2 nM, hCA II with K-i values of 298.9 +/- 55.7-926.1 +/- 330.0 nM, alpha-glycosidase with K-i values of 170.3 +/- 27-760.1 +/- 269 mu M, AChE with K-i values of 27.1 +/- 3-77.6 +/- 1.7 nM, and BChE with K-i values of 21.0 +/- 5-61.3 +/- 15 nM. As a result, novel vinyl functionalized 5,6-dimethylbenzimidazolium salts (1a-g) exhibited effective inhibition profiles toward studied metabolic enzymes. Therefore, we believe that these results may contribute to the development of new drugs particularly to treat some global disorders including glaucoma, Alzheimer's disease, and diabetes.
Açıklama
Anahtar Kelimeler
5,6-dimethylbenzimidazolium salts, acetylcholinesterase, butyrylcholinesterase, carbonic anhydrase, enzyme inhibition, alpha-glycosidase
Kaynak
Journal of Biochemical and Molecular Toxicology
WoS Q Değeri
Q2
Scopus Q Değeri
Q2
Cilt
37
Sayı
2
