期刊
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
卷 17, 期 10, 页码 -出版社
MDPI
DOI: 10.3390/ijms17101736
关键词
carbonic anhydrase; acetylcholinesterase; beta-lactam; 2-azetidinone; enzyme inhibition; enzyme purification
资金
- Sakarya University [BAPK-2012-02-04-031]
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.
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