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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.
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页码:6509 / 6514
页数:6
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