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含吡唑的新型1,2,4-三唑并[3,4-b][1,3,4]噻二唑类化合物作为强效抗菌剂的合成。

Synthesis of new 1,2,4-triazole[3,4-b][1,3,4]thiadiazoles bearing pyrazole as potent antimicrobial agents.

作者信息

Sanjeeva Reddy Cherkupally, Sanjeeva Rao Lade, Rajesh Kumar Gaddam, Nagaraj Adki

机构信息

Department of Chemistry, Kakatiya University, Warangal–506 009, India.

出版信息

Chem Pharm Bull (Tokyo). 2010 Oct;58(10):1328-31. doi: 10.1248/cpb.58.1328.

Abstract

A new series of 6-(aryl/heteryl)-3-(5-methyl-1-phenyl-1H-4-pyrazolyl)[1,2,4]triazolo[3,4-b][1,3,4]thiadiazoles (7a-j) has been synthesized by the reaction of 4-amino-5-(5-methyl-1-phenyl-1H-4-pyrazolyl)-4H-1,2,4-triazol-3-yl-hydrosulfide (6) with POCl(3) and the corresponding aryl/heteryl carboxylic acid, in ethanol at reflux temperature for 12 h. All the synthesized compounds were tested for in vitro activities against certain strains of bacteria such as Staphylococcus aureus, Bacillus subtilis, Escherichia coli and fungi such as Aspergillus niger, Aspergillus nodulans, Alternaria alternate. Compounds having 4-chlorophenyl (7d), 4-aminophenyl (7f), 4-nitrophenyl (7h) and 3-pyridyl (7i) substituents at 6-position of thiadiazole ring, showed marked inhibition of bacterial and fungal growth nearly equal to the standards. The other new compounds also showed appreciable activity against the test bacteria and fungi.

摘要

通过使4-氨基-5-(5-甲基-1-苯基-1H-4-吡唑基)-4H-1,2,4-三唑-3-基氢硫化物(6)与POCl₃及相应的芳基/杂芳基羧酸在乙醇中于回流温度反应12小时,合成了一系列新的6-(芳基/杂芳基)-3-(5-甲基-1-苯基-1H-4-吡唑基)[1,2,4]三唑并[3,4-b][1,3,4]噻二唑(7a-j)。对所有合成化合物进行了体外抗某些细菌菌株(如金黄色葡萄球菌、枯草芽孢杆菌、大肠杆菌)和真菌菌株(如黑曲霉、结节曲霉、链格孢)活性的测试。在噻二唑环6-位具有4-氯苯基(7d)、4-氨基苯基(7f)、4-硝基苯基(7h)和3-吡啶基(7i)取代基的化合物,对细菌和真菌生长显示出显著抑制,几乎与标准品相当。其他新化合物对受试细菌和真菌也表现出可观的活性。

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