4.7 Article

Synthesis of triazole Schiff bases: Novel inhibitors of nucleotide pyrophosphatase/phosphodiesterase-1

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BIOORGANIC & MEDICINAL CHEMISTRY
卷 22, 期 22, 页码 6509-6514

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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

  1. Higher Education Commission (HEC), Pakistan under the 'National Research Program for Universities' [20-1910]
  2. HEC 5000 indigenous fellowship program

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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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