Synthesis and antibacterial activity of some 5-guanylhydrazone/thiocyanato-6-arylimidazo[2,1-b]-1,3,4-thiadiazole-2-sulfonamide derivatives

被引：228

作者：

Gadad, AK ^{[1
]}

Mahajanshetti, CS ^{[1
]}

Nimbalkar, S ^{[1
]}

Raichurkar, A ^{[1
]}

机构：

[1] Coll Pharm, Dept Med Chem, Belgaum 590010, India

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2000年 / 35卷 / 09期

关键词：

5-guanylhydrazone; thiocyanatoimidazo[2,1-b]-1,3,4-thiadiazoles-2-sulfonamides; synthesis; antibacterial activity;

D O I：

10.1016/S0223-5234(00)00166-5

中图分类号：

R914 [药物化学];

学科分类号：

100701 [药物化学];

摘要：

6-Arylimidazo[2,1-b]-1,3,4-thiadiazole-2-sulfonamides 3 on Vilsmeier-Haak reaction produced 5-formyl-6-arylimidazo[2, 1-b]1,3,3-thiadiazole-2-[N-(dimethylaminomethino)]sulfonamides 4, while 3 on treatment with potassium thiocyanate in the presence of bromine in acetic acid produced 5-thiocyanato-2-sulfonamides 6. Interaction of 4 with aminoguanidine hydrochloride in ethanol produced the corresponding 5-guanylhydrazone derivatives 5. Compounds 5 and 6 showed a high degree of antibacterial activity against both Escherichia coli and Staphylococcus aureus comparable to that of sulfamethoxazole and Norfloxacin. However, they were found to show moderate activity against Salmonella typhi, Pseudomonas aeruginosa and Pneumococci. (C) 2000 Editions scientifiques et medicales Elsevier SAS.

引用

页码：853 / 857

页数：5

共 10 条

[1]

SYNTHESIS AND MITOGENIC ACTIVITY OF NEW IMIDAZO[2,1-B]THIAZOLES [J].