n -环烷基基-2-酰基烷基基-2,3-二氢-1,3-苯并噻唑的结构修饰和抗菌活性

Andrea Latrofa, Massimo Franco, Angela Lopedota, Antonio Rosato, Dora Carone, Cesare Vitali
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引用次数: 33

摘要

合成了一系列n -环烷基基-2-酰基烷基基-2,3-二氢-1,3-苯并噻唑5a-j、n -环烷基基-2-酰基烷基基-2,3-二氢-1,3-苯并噻唑8a-e和n -烷基基-2-酰基烷基基-2,3-二氢-1,3-苯并噻唑8f-h,并对4种革兰氏阴性菌(枯草芽孢杆菌6633、粪肠球菌29212、金黄色葡萄球菌6538、金黄色葡萄球菌25923、大肠杆菌25922、钙溶性不动杆菌a1、钙溶性假单胞菌a2、铜绿假单胞菌27835、氧化克雷伯菌49131)、4种酵母样真菌和1种真菌(热带念珠菌750、白色念珠菌14053、白色念珠菌10231、laurencoccus 18803和酿酒酵母)。采用微量稀释肉汤法和琼脂稀释法进行抑菌试验。结果表明,部分化合物5和8对某些细菌菌株有效,而只有化合物8b-g对所评价的酵母菌株表现出中等的抗真菌活性。
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Structural modifications and antimicrobial activity of N-cycloalkenyl-2-acylalkylidene-2,3-dihydro-1,3-benzothiazoles

A series of N-cycloalkenyl-2-acylalkylidene-2,3-dihydro-1,3-benzothiazoles 5aj, N-cycloalkyl-2-acylalkylidene-2,3-dihydro-1,3-benzothiazoles 8ae, and N-alkyl-2-acylalkylidene-2,3-dihydro-1,3-benzothiazoles 8fh, were synthesized and tested for in vitro antibacterial and antifungal activities against four gram-positive and five gram-negative bacteria (Bacillus subtilis 6633, Enterococcus faecalis 29212, Staphylococcus aureus 6538, Staphylococcus aureus 25923, Escherichia coli 25922, Acinetobacter calcoaceticus a1, A. calcoaceticus a2, Pseudomonas aeruginosa 27835, Klebsiella oxytoca 49131), four yeast-like fungi and one fungus (Candida tropicalis 750, C. albicans 14053, C. albicans 10231, Criptococcus laurentii 18803, and Saccharomyces cerevisiae). Microdilution broth and agar dilution methods were used for antimicrobial tests. The findings obtained showed that some of the tested compounds 5 and 8 were effective against some of the bacterial strains used, whereas, only compounds 8bg exhibited a moderate antifungal activity against the yeast strains evaluated.

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