Synthesis and biological evaluation of phloroglucinol derivatives possessing α-glycosidase, acetylcholinesterase, butyrylcholinesterase, carbonic anhydrase inhibitory activity

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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.

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Burmaoglu, S., Yilmaz, A. O., Taslimi, P., Algul, O., Kilic, D., & Gulcin, I. (2018). Synthesis and biological evaluation of phloroglucinol derivatives possessing α-glycosidase, acetylcholinesterase, butyrylcholinesterase, carbonic anhydrase inhibitory activity. Archiv Der Pharmazie, 351(2). https://doi.org/10.1002/ardp.201700314

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