Synthesis and Antimicrobial Activities of N-(Heteroaryl-substituted)-p-toluenesulphonamides

Ozoh Chinwe Francisca, O. U. Chris, Ugwu D. Izuchukwu
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Abstract

A new class of N-(heteroaryl-substituted)-p-toluenesulphonamides has been synthesized exhibiting antibacterial and antifungal properties. The condensation reaction of p-toluenesulphonyl chloride 1 with appropriate substituted amino pyridines 2a–g in acetone furnished N-(heteroaryl-substituted)-p-toluenesulphonamides 3a–g. These derivatives were characterized by IR, 1H-, and 13C-NMR spectroscopy and were screened in vitro against gram-positive bacteria, gram-negative bacteria, and fungi organisms using agar-diffusion method. Results indicated improved biological activities over reference drugs such as Tetracycline (TCN) and Fluconazole (FLU).
N-(杂芳基取代)-对甲苯磺酰胺的合成及抗菌活性研究
合成了一类新的N-(杂芳基取代)-对甲苯磺酰胺类化合物,具有抗菌和抗真菌的作用。对甲苯磺酰氯1与适当取代的氨基吡啶2a-g在提供N-(杂芳基取代)-对甲苯磺酰胺3a-g的丙酮中缩合反应。通过IR, 1H-和13C-NMR对这些衍生物进行了表征,并利用琼脂扩散法对革兰氏阳性菌,革兰氏阴性菌和真菌生物进行了体外筛选。结果表明,与四环素(TCN)和氟康唑(FLU)等参比药物相比,其生物活性有所提高。
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