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Synthesis and biological evaluation of phloroglucinol derivatives possessing α‐glycosidase,acetylcholinesterase, butyrylcholinesterase,carbonic anhydrase inhibitory activity
Authors:Serdar Burmaoglu  Ali O. Yilmaz  Parham Taslimi  Oztekin Algul  Deryanur Kilic  Ilhami Gulcin
Affiliation:1. Faculty of Science, Department of Chemistry, Ataturk University, Erzurum, Turkey;2. Tercan Vocational High School, Erzincan University, Erzincan, Turkey;3. Faculty of Pharmacy, Department of Pharmaceutical Chemistry, Mersin University, Mersin, Turkey;4. Faculty of Art and Science, Department of Chemistry, Aksaray University, Aksaray, Turkey
Abstract:
A series of novel phloroglucinol derivatives were designed, synthesized, characterized spectroscopically and tested for their inhibitory activity against selected metabolic enzymes, including α‐glycosidase, acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and human carbonic anhydrase I and II (hCA I and II). These compounds displayed nanomolar inhibition levels and showed Ki values of 1.14–3.92 nM against AChE, 0.24–1.64 nM against BChE, 6.73–51.10 nM against α‐glycosidase, 1.80–5.10 nM against hCA I, and 1.14–5.45 nM against hCA II.
Keywords:α  ‐glycosidase  acetylcholinesterase  butyrylcholinesterase  carbonic anhydrase  phloroglucinol derivatives
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