期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 22, 期 22, 页码 6509-6514出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2014.08.032
关键词
Nucleotide pyrophosphatase/phosphodiesterase-1; Schiff bases of triazoles; PC3 cell lines; Chondrocalcinosis
资金
- Higher Education Commission (HEC), Pakistan under the 'National Research Program for Universities' [20-1910]
- HEC 5000 indigenous fellowship program
A series of Schiff base triazoles 1-25 was synthesized and evaluated for their nucleotide pyrophosphatase/ phosphodiesterase-1 inhibitory activities. Among twenty-five compounds, three compounds 10 (IC50 = 132.20 +/- 2.89 mu M), 13 (IC50 = 152.83 +/- 2.39 mu M), and 22 (IC50 = 251.0 +/- 6.64 mu M) were identified as potent inhibitors with superior activities than the standard EDTA (IC50 = 277.69 +/- 2.52 mu M). The newly identified inhibitors may open a new avenue for the development of treatment of phosphodiesterase-I related disorders. These compounds were also evaluated for carbonic anhydrase, acetylcholinesterase and butyrylcholinesterase inhibitory potential and were found to be inactive. The compounds showed non-toxic effect towards PC3 cell lines. (C) 2014 Elsevier Ltd. All rights reserved.
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