期刊
ARCHIV DER PHARMAZIE
卷 351, 期 10, 页码 -出版社
WILEY-V C H VERLAG GMBH
DOI: 10.1002/ardp.201800200
关键词
acetylcholinesterase; butyrylcholinesterase; carbonic anhydrase; enzyme inhibition; substituted pyrazol-4-yl-diazene
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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