Bioorganic & Medicinal Chemistry 2014-11-15

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

Khalid Mohammed Khan, Salman Siddiqui, Muhammad Saleem, Muhammad Taha, Syed Muhammad Saad, Shahnaz Perveen, M Iqbal Choudhary

文献索引：Bioorg. Med. Chem. 22(22) , 6509-14, (2015)

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摘要

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 lM), 13 (IC50 = 152.83 ± 2.39 lM), and 22 (IC50 = 251.0 ± 6.64 lM) were identified as potent inhibitors with superior activities than the standard EDTA (IC50 = 277.69 ± 2.52 lM). 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.