作为抗菌剂的一系列苯并噻唑酰胺的合成、表征和体外生物学评价

Q4 Chemistry
Hadyah Mohammed Alazmaa, V. Avupati, Carolina Santiago
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引用次数: 0

摘要

利用改良的肖滕-鲍曼反应条件合成了一系列苯并噻唑酰胺(VH01-06),所有化合物的收率和纯度都很高。利用物理和光谱方法对这些化合物的分子结构进行了表征。化合物的结构与 FT-IR、1H NMR、13C NMR 和 HRMS ESI-Mass 光谱技术获得的分析数据一致。此外,化合物还对各种菌株进行了体外抗菌活性筛选,包括革兰氏阳性菌(耐甲氧西林金黄色葡萄球菌(MRSA)ATCC 3359 和甲氧西林敏感金黄色葡萄球菌(MSSA)ATCC 2592)和革兰氏阴性菌(大肠杆菌 J53 R1、大肠杆菌 ATCC 2592 和大肠杆菌 J53 R1)、大肠杆菌 ATCC 25922、肺炎克雷伯菌 ATCC 10031 和肺炎克雷伯菌 BAA-1075)。根据生物筛选结果,发现 VH01-06 化合物对所选菌株的抗菌性能有限,因为所记录的活性是在 100 µM 浓度时发现的。而化合物 VH05 在 200 µg/mL 浓度下对大肠杆菌 ATCC 25923 具有特异性活性。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Synthesis, Characterization, in vitro Biological Evaluation of a Series of Benzothiazole Amides as Antibacterial Agents
A series of benzothiazole amides (VH01-06) were synthesized by using modified Schotten-Baumann reaction conditions, all the resultant compounds were obtained in good yields and purity. The molecular structure of the compounds was characterized using physical and spectral methods. The structures of the compounds were consistent with the analytical data obtained for FT-IR, 1H NMR, 13C NMR and HRMS ESI-Mass spectroscopic techniques. Further, compounds were subjected to the in vitro antibacterial activity screening against various strains that includes Gram-positive bacteria (methicillin-resistant Staphylococcus aureus (MRSA) ATCC 3359 and methicillin-sensitive Staphylococcus aureus (MSSA) ATCC 2592) and Gram-negative bacteria (Escherichia coli J53 R1, Escherichia coli ATCC 25922, Klebsiella pneumoniae ATCC 10031 and Klebsiella pneumonia BAA-1075). Based on the biological screening results, compounds VH01-06 were found to possesses limited antibacterial properties against selected strains, since the recorded activity was found at 100 µM concentration. While compound VH05 displayed specific activity against E. coli ATCC 25923 at 200 µg/mL.
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来源期刊
Asian Journal of Chemistry
Asian Journal of Chemistry 化学-化学综合
CiteScore
0.80
自引率
0.00%
发文量
229
审稿时长
4 months
期刊介绍: Information not localized
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