Catalytic derivatization of 2-Aminobenzo[d]thiazole for observing antibacterial activity and in silico analysis

S. Bepary, B. K. Biswas, F. M. Nazia, S. Islam, T. S. Juthy
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Abstract

2-Aminobenzo[d]thiazoles have been converted to corresponding acetanilides and 2-hydroxy compounds for observing antibacterial activities. The acetylation was done by direct use of acetic acid, whereas the corresponding 2-hydroxy derivative was synthesized following various reaction conditions with or without a catalyst for observing the associated yield and ease of the reaction. In this study, the reaction yield was found to be between 20% and 86%. The synthesized acetanilides and the 2-hydroxy compounds were screened for antibacterial activity against various common pathogenic gram-positive and gram-negative organisms. Encouraging antimicrobial potential was noted from these small molecules. Finally, the compounds were taken for in silico analysis to observe the possible orientations in the binding site of the alanine racemase enzyme of Enterococcus faecalis.
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2-氨基苯并[d]噻唑的催化衍生化及其抑菌活性观察和硅分析
2-氨基苯并[d]噻唑被转化为相应的乙酰苯胺和2-羟基化合物,以观察抗菌活性。直接用乙酸进行乙酰化反应,在不同的反应条件下合成相应的2-羟基衍生物,观察反应的产率和难易程度。在本研究中,发现反应收率在20% ~ 86%之间。对合成的乙酰苯胺及其2-羟基化合物进行了抗菌活性筛选,测定其对多种常见致病性革兰氏阳性和革兰氏阴性菌的抑菌活性。从这些小分子中发现了令人鼓舞的抗菌潜力。最后,对化合物进行硅晶分析,观察粪肠球菌丙氨酸消旋酶结合位点的可能取向。
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38
审稿时长
15 weeks
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