Discovery of Potent Carbonic Anhydrase and Acetylcholinesterase Inhibitors: 2-Aminoindan beta-Lactam Derivatives

Genc, Hayriye; Kalin, Ramazan; KÖKSAL, ZEYNEP; SADEGHIAN, Nastaran; KOÇYİĞİT, ÜMİT MUHAMMET; Zengin, Mustafa; Gülçin, İlhami; Özdemir, Hasan

doi:10.3390/ijms17101736

Makale Tam Makale Uluslararası 2016

Discovery of Potent Carbonic Anhydrase and Acetylcholinesterase Inhibitors: 2-Aminoindan beta-Lactam Derivatives

Hayriye Genc, Ramazan Kalin, ZEYNEP KÖKSAL, Nastaran SADEGHIAN, ÜMİT MUHAMMET KOÇYİĞİT, Mustafa Zengin, İlhami Gülçin, Hasan Özdemir

International Journal of Molecular Sciences Cilt 17 · Sayı 10 · 01.10.2016

DOI ile aç

Özet

beta-Lactams are pharmacologically important compounds because of their various biological uses, including antibiotic and so on. beta-Lactams were synthesized from benzylidene-inden derivatives and acetoxyacetyl chloride. The inhibitory effect of these compounds was examined for human carbonic anhydrase I and II (hCA I, and II) and acetylcholinesterase (AChE). The results reveal that beta-lactams are inhibitors of hCA I, II and AChE. The Ki values of beta-lactams (2a-k) were 0.44-6.29 nM against hCA I, 0.93-8.34 nM against hCA II, and 0.25-1.13 nM against AChE. Our findings indicate that beta-lactams (2a-k) inhibit both carbonic anhydrases (CA) isoenzymes and AChE at low nanomolar concentrations.

Anahtar kelimeler

carbonic anhydrase phenolic compounds Acetylcholinesterase enzyme inhibition SULFONAMIDE DERIVATIVES ENZYME-ACTIVITY PURIFICATION VITRO SULFAMIDES ERYTHROCYTE ISOZYMES I enzyme purification Lactoperoxidase beta-lactam 2-azetidinone ISOENZYMES HCA I ESTERASE INHIBITORS

Atıf için künye

Genc, H., Kalin, R., KÖKSAL, Z., SADEGHIAN, N., KOÇYİĞİT, Ü. M., Zengin, M., Gülçin, İ., & Özdemir, H. (2016). Discovery of Potent Carbonic Anhydrase and Acetylcholinesterase Inhibitors: 2-Aminoindan beta-Lactam Derivatives. International Journal of Molecular Sciences, 17(10). https://doi.org/10.3390/ijms17101736

BibTeX

@article{genc2016-67327,
  author = {Genc, Hayriye and Kalin, Ramazan and KÖKSAL, ZEYNEP and SADEGHIAN, Nastaran and KOÇYİĞİT, ÜMİT MUHAMMET and Zengin, Mustafa and Gülçin, İlhami and Özdemir, Hasan},
  title = {Discovery of Potent Carbonic Anhydrase and Acetylcholinesterase Inhibitors: 2-Aminoindan beta-Lactam Derivatives},
  journal = {International Journal of Molecular Sciences},
  year = {2016},
  volume = {17},
  number = {10},
  issn = {1661-6596},
  doi = {10.3390/ijms17101736},
  url = {https://akademik.atauni.edu.tr/yayinlar/67327-discovery-of-potent-carbonic-anhydrase-and-acetylcholinesterase-inhibitors-2}
}