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Some pyrazoles derivatives: Potent carbonic anhydrase, α‐glycosidase, and cholinesterase enzymes inhibitors
Author(s) -
Turkan Fikret,
Cetin Adnan,
Taslimi Parham,
Gulçin İlhami
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.201800200
Subject(s) - carbonic anhydrase , butyrylcholinesterase , chemistry , aché , acetylcholinesterase , enzyme , cholinesterase , carbonic anhydrase i , biochemistry , pharmacology , biology
A series of substituteed pyrazol‐4‐yl‐diazene derivatives were found to be effective inhibitors against α‐glycosidase, cytosolic carbonic anhydrase I and II isoforms (hCA I and II), butyrylcholinesterase (BChE), and acetylcholinesterase (AChE) with K i values in the range of 33.72 ± 7.93 to 90.56 ± 27.52 nM for α‐glycosidase, 1.06 ± 0.16 to 9.83 ± 0.74 nM for hCA I, 0.68 ± 0.12 to 7.16 ± 1.14 nM for hCA II, 44.66 ± 10.06 to 78.34 ± 17.83 nM for AChE, and 50.36 ± 13.88 to 88.36 ± 20.03 nM for BChE, respectively. Recently, inhibition of these metabolic enzymes has been considered as a promising factor for pharmacologic intervention in a diversity of disturbances, such as diabetes, glaucoma, obesity, epilepsy, cancer, and neurodegenerative diseases.