Synthesis, antioxidant activities and urease inhibition of some new 1,2,4-triazole and 1,3,4-thiadiazole derivatives

被引:304
作者
Khan, Imtiaz [1 ]
Ali, Sajid [1 ]
Hameed, Shahid [1 ]
Rama, Nasim Hasan [1 ]
Hussain, Muhammad Tahir [2 ]
Wadood, Abdul [3 ]
Uddin, Reaz [3 ]
Ul-Haq, Zaheer [3 ]
Khan, Ajmal [3 ]
Ali, Sajjad [3 ]
Choudhary, M. Iqbal [3 ]
机构
[1] Quaid I Azam Univ, Dept Chem, Islamabad 45320, Pakistan
[2] Natl Text Univ, Dept Appl Sci, Faisalabad 37610, Pakistan
[3] Univ Karachi, Int Ctr Chem & Biol Sci, Dr Panjwani Ctr Mol Med & Drug Res, Karachi 75270, Pakistan
关键词
1,2,4-Triazoles; 1,3,4-Thiadiazoles; Antioxidant activities; Urease inhibition; POTATO;
D O I
10.1016/j.ejmech.2010.08.034
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
New series of 4,5-disubstituted-2,4-dihydro-3H-1,2,4-triazole-3-thiones (8a-j) and 2,5-disubstituted-1,3,4-thiadiazoles (9a-h) were synthesized by dehydrative cyclization of hydrazinecarbothioamide derivatives (7a-k) by refluxing in 4 N aqueous sodium hydroxide and by overnight stirring with polyphosphoric acid, respectively. The structures of the newly synthesized compounds were characterized by IR, H-1 NMR, C-13 NMR, elemental analysis and mass spectroscopic studies and the synthesized compounds were screened for their antioxidant and urease inhibition activities. N-(2,4-Dimethylphenyl)-5-(4-nitrophenyl)-1,3,4-thiadiazol-2-amine (9h) showed excellent antioxidant activity more than the standard drug whereas 4-(2,4-dimethylphenyl)-5-(3-nitrophenyl)-2,4-dihydro-3H-1,2,4-triazole-3-thione (8d) and 4-(2,3-dimethylphenyl)-5-phenyl-2,4-dihydro-3H-1,2,4-triazole-3-thione (8e) exhibited potent urease inhibitory activities. (C) 2010 Elsevier Masson SAS. All rights reserved.
引用
收藏
页码:5200 / 5207
页数:8
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