Some pyrazoles derivatives: Potent carbonic anhydrase, -glycosidase, and cholinesterase enzymes inhibitors

被引：69
作者：
Turkan, Fikret [1 ]
Cetin, Adnan [2 ]
Taslimi, Parham [3 ]
Gulcin, Ilhami [3 ]
机构：
[1] Igdir Univ, Hlth Serv Vocat Sch, Igdir, Turkey
[2] Mus Alparslan Univ, Dept Sci, Fac Educ, Mus, Turkey
[3] Ataturk Univ, Dept Chem, Fac Sci, TR-25240 Erzurum, Turkey
来源：
ARCHIV DER PHARMAZIE | 2018年 / 351卷 / 10期
关键词：
acetylcholinesterase; butyrylcholinesterase; carbonic anhydrase; enzyme inhibition; substituted pyrazol-4-yl-diazene; INCLUDING NATURAL-PRODUCTS; GLUTATHIONE-S-TRANSFERASE; ALPHA-GLUCOSIDASE; 1ST SYNTHESIS; ACETYLCHOLINESTERASE; BUTYRYLCHOLINESTERASE; PROFILES; ANTIOXIDANT; BROMOPHENOLS; BENZENESULFONAMIDES;
D O I：
10.1002/ardp.201800200
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A series of substituteed pyrazol-4-yl-diazene derivatives were found to be effective inhibitors against -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 +/- 27.52nM for -glycosidase, 1.06 +/- 0.16 to 9.83 +/- 0.74nM for hCA I, 0.68 +/- 0.12 to 7.16 +/- 1.14nM for hCA II, 44.66 +/- 10.06 to 78.34 +/- 17.83nM for AChE, and 50.36 +/- 13.88 to 88.36 +/- 20.03nM 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.
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页数：7
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