Discovery of Potent Carbonic Anhydrase and Acetylcholinesterase Inhibitors: 2-Aminoindan beta-Lactam Derivatives
Date
2016Author
Genc, HayriyeKalin, Ramazan
Koksal, Zeynep
Sadeghian, Nastaran
Kocyigit, Umit M.
Zengin, Mustafa
Gulcin, Ilhami
Ozdemir, Hasan
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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.
Source
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCESVolume
17Issue
10Collections
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