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Synthesis and biological evaluation of phloroglucinol derivatives possessing α‐glycosidase, acetylcholinesterase, butyrylcholinesterase, carbonic anhydrase inhibitory activity
Author(s) -
Burmaoglu Serdar,
Yilmaz Ali O.,
Taslimi Parham,
Algul Oztekin,
Kilic Deryanur,
Gulcin Ilhami
Publication year - 2018
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.201700314
Subject(s) - butyrylcholinesterase , acetylcholinesterase , chemistry , carbonic anhydrase , aché , phloroglucinol , enzyme , carbonic anhydrase i , cholinesterase , stereochemistry , biochemistry , inhibitory postsynaptic potential , carbonic anhydrase ii , organic chemistry , pharmacology , biology , neuroscience
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 K i 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.