Synthesis And Antibacterial Activities Of Benzothiazole Derivatives Of Sulphonamides

C. B. Ikpa, S. Onoja, Anastasia O. Okwaraji
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引用次数: 5

Abstract

Abstract This study aims to synthesize hybrid compounds “via” the coupling of sulphonamide and benzothiazole into one structure that may have improved antibacterial property. The N-(biphenyl-4-yl) thiourea (1) used for the synthesis of the targeted sulphonamides was obtained by reacting diphenylamine and ammonium thiocyanate at room temperature. Cyclization of N-(biphenyl-4-yl)thiourea gave 2-amino-6-phenylbenzothiazole (2) which reacted with benzenesulphonyl chloride and para-toulene sulphonyl chloride to give the targeted sulphonamides (3a & 3b). The synthesized compounds were characterised using melting point, infra-red spectroscopy, nuclear magnetic resonance and elemental analysis. Anti-bacterial screening of the synthesised compounds indicated that all the compounds showed anti-bacterial properties, except 2-amino-6-phenylbenzothiazole that did not show any activity on Escherichia coli.
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磺胺类苯并噻唑类衍生物的合成及抗菌活性研究
摘要本研究旨在“通过”磺胺与苯并噻唑的偶联合成一种可能具有更好抗菌性能的杂化化合物。二苯胺与硫氰酸铵在室温下反应得到用于合成目标磺胺类化合物的N-(联苯-4-基)硫脲(1)。N-(联苯-4-基)硫脲环化得到2-氨基-6-苯基苯并噻唑(2),它与苯磺酰氯和对甲苯磺酰氯反应得到目标磺胺(3a和3b)。用熔点、红外光谱、核磁共振和元素分析对合成的化合物进行了表征。抗菌筛选结果表明,除2-氨基-6-苯基苯并噻唑对大肠杆菌无抑制作用外,其余化合物均具有抗菌活性。
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