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

被引:39
|
作者
Khan, Khalid Mohammed [1 ]
Siddiqui, Salman [1 ]
Saleem, Muhammad [1 ]
Taha, Muhammad [1 ,2 ]
Saad, Syed Muhammad [1 ]
Perveen, Shahnaz [3 ]
Choudhary, M. Iqbal [1 ,4 ]
机构
[1] Univ Karachi, HEJ Res Inst Chem, Int Ctr Chem & Biol Sci, Karachi 75270, Pakistan
[2] Univ Teknol MARA UiTM, Atta ur Rahman Inst Nat Prod Discovery, Bandar Puncak Alam 42300, Selangor, Malaysia
[3] Shahrah e Dr Salimuzzaman Siddiqui, PCSIR Labs Complex, Karachi 75280, Pakistan
[4] King Abdulaziz Univ, Fac Sci, Dept Biochem, Jeddah 21412, Saudi Arabia
关键词
Nucleotide pyrophosphatase/phosphodiesterase-1; Schiff bases of triazoles; PC3 cell lines; Chondrocalcinosis; DERIVATIVES; PHOSPHODIESTERASE; ANTICANCER; GLYCOSIDES; DRUGS;
D O I
10.1016/j.bmc.2014.08.032
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
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 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.
引用
收藏
页码:6509 / 6514
页数:6
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