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

ABSTRACT: ?-Lactams are pharmacologically important compounds because of their various biological uses, including antibiotic and so on. ?-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 ?-lactams are inhibitors of hCA I, II and AChE. The Ki values of ?-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 ?-lactams (2a-k) inhibit both carbonic anhydrases (CA) isoenzymes and AChE at low nanomolar concentrations.

SUBMITTER: Genc H 

PROVIDER: S-EPMC5085765 | biostudies-literature | 2016 Oct

REPOSITORIES: biostudies-literature

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

Genç Hayriye H   Kalin Ramazan R   Köksal Zeynep Z   Sadeghian Nastaran N   Kocyigit Umit M UM   Zengin Mustafa M   Gülçin İlhami İ   Özdemir Hasan H  

International journal of molecular sciences 20161020 10

β-Lactams are pharmacologically important compounds because of their various biological uses, including antibiotic and so on. β-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 β-lactams are inhibitors of hCA I, II and AChE. The <i>K<sub>i</sub></i> values of β-lactams (<b>2a</b>-<b>k</b>) were  ...[more]

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