Published January 1, 2018 | Version v1
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Synthesis and biological evaluation of phloroglucinol derivatives possessing -glycosidase, acetylcholinesterase, butyrylcholinesterase, carbonic anhydrase inhibitory activity

  • 1. Ataturk Univ, Dept Chem, Fac Sci, Erzurum, Turkey
  • 2. Mersin Univ, Dept Pharmaceut Chem, Fac Pharm, Mersin, Turkey
  • 3. Aksaray Univ, Fac Art & Sci, Dept Chem, Aksaray, Turkey

Description

A series of novel phloroglucinol derivatives were designed, synthesized, characterized spectroscopically and tested for their inhibitory activity against selected metabolic enzymes, including -glycosidase, acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and human carbonic anhydrase I and II (hCA I and II). These compounds displayed nanomolar inhibition levels and showed K-i values of 1.14-3.92nM against AChE, 0.24-1.64nM against BChE, 6.73-51.10nM against -glycosidase, 1.80-5.10nM against hCA I, and 1.14-5.45nM against hCA II.

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