Reddy Cherkupally Sanjeeva, Rao Dasari Chandrasekhar, Yakub Vookanti, Nagaraj Adki
Acta Chim Slov. 2011 Sep;58(3):582-9.
A new series of novel bis[1, 2, 4]triazolo[3, 4-b][1, 3, 4]thiadiazines 7a-j has been synthesized by the reaction of [5, 5'-methylenebis(3-methylbenzofuran-7, 5-diyl)]bis[(4-amino-5-thioxo-4, 5-dihydro-1H-1, 2, 4-triazol-3-yl)methanone] (6) with a variety of phenacyl bromides in ethanol under reflux for 6 h. All the newly synthesized compounds were tested for in vitro activity against certain strains of bacteria such as Escherichia coli, Klebsiella pneumoniae, Shigella dysenteriae and Shigella flexneri. Compounds 7a, 7c and 7g were highly active against the entire organism employed. Compound 7c showed the activity higher than the standard drug neomycin, and almost equal to the streptomycin. Compounds 7a-j were also screened for their antifungal activity against Aspergillus niger, Candida albicans, Aspergillus flavus and Rhizopus oryzae. Compounds with methoxyphenyl moiety 7d and dichlorophenyl moiety 7f showed significant activity against the tested fungal strains.
通过[5, 5'-亚甲基双(3-甲基苯并呋喃-7, 5-二基)]双(4-氨基-5-硫代-4, 5-二氢-1H-1, 2, 4-三唑-3-基)甲酮与多种苯甲酰溴在乙醇中回流反应6小时，合成了一系列新型双[1, 2, 4]三唑并[3, 4-b][1, 3, 4]噻二嗪7a - j。对所有新合成的化合物进行了体外抗某些细菌菌株的活性测试，如大肠杆菌、肺炎克雷伯菌、痢疾志贺菌和福氏志贺菌。化合物7a、7c和7g对所使用的所有生物体均具有高活性。化合物7c显示出高于标准药物新霉素的活性，且几乎与链霉素相当。还对化合物7a - j进行了抗黑曲霉、白色念珠菌、黄曲霉和米根霉的抗真菌活性筛选。带有甲氧基苯基部分的化合物7d和带有二氯苯基部分的化合物7f对测试的真菌菌株显示出显著活性。
