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

被引：297

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

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2010年 / 45卷 / 11期

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

页码：5200 / 5207

页数：8

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