Synthesis and biological evaluation of novel 4-(6-substituted quinolin-4-yl)-N-aryl thiazol-2-amine derivatives as potential antimicrobial agents,Journal of Heterocyclic Chemistry

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Synthesis and biological evaluation of novel 4-(6-substituted quinolin-4-yl)-N-aryl thiazol-2-amine derivatives as potential antimicrobial agents
Journal of Heterocyclic Chemistry ( IF 2.0 ) Pub Date : 2021-06-04 , DOI: 10.1002/jhet.4317
Prashant Thakare ₁ , Abhijit Shinde ₁ , Sagar Dhakane ₂ , Abhijit Chavan ₁ , Vivek Bobade ₃ , Pravin C. Mhaske ₁

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Cyclocondensation reaction of 4-(2-bromoacetyl)quinolin-1-ium bromide (4a–d) with substituted arylthiourea, (5a–g) afforded 4-(6-substituted quinolin-4-yl)-N-aryl/pyridyl thiazol-2-amine (6a-ab). These newly synthesized derivatives were evaluated for in vitro antibacterial activity against Escherichia coli (NCIM 2574), Proteus mirabilis (NCIM 2388) (Gram-negative strains), Bacillus subtilis (NCIM 2063), Staphylococcus albus (NCIM 2178) (Gram-positive strains) and in vitro antifungal activity against Aspergillus niger (ATCC 504) and Candida albicans (NCIM 3100). Compounds 6a, 6b, 6d, 6f, 6k, and 6l showed moderate to good antibacterial activity against S. albus. Ten derivatives 6c, 6q, 6r, 6s, 6t, 6v, 6w, 6x, 6y, and 6aa, showed moderate to good activity against A. niger. N-[4-(Quinolin-4-yl)-1,3-thiazol-2-yl]pyridin-2-amine presented comparable activity against A. niger with respect to standard drug Rouconazole.

中文翻译：

新型 4-(6-取代喹啉-4-基)-N-芳基噻唑-2-胺衍生物作为潜在抗菌剂的合成和生物学评价

4-（2-溴乙酰基）喹啉-1-鎓溴化物（4a-d）与取代的芳基硫脲（5a-g）的环缩聚反应得到4-（6-取代的喹啉-4-基）-N-芳基/吡啶基噻唑-2-胺（6a-ab）。评估了这些新合成的衍生物对大肠杆菌（NCIM 2574）、奇异变形杆菌（NCIM 2388）（革兰氏阴性菌株）、枯草芽孢杆菌（NCIM 2063）、白色葡萄球菌（NCIM 2178）（革兰氏阳性菌株）的体外抗菌活性) 和体外对黑曲霉的抗真菌活性(ATCC 504) 和白色念珠菌(NCIM 3100)。化合物6a、6b、6d、6f、6k和6l对S. albus显示出中等至良好的抗菌活性。10 种衍生物6c、6q、6r、6s、6t、6v、6w、6x、6y和6aa对A. niger显示出中等至良好的活性。N- [4-(Quinolin-4-yl)-1,3-thiazol-2-yl]pyridin-2-amine 对A. niger相对于标准药物鲁康唑。

更新日期：2021-06-04

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