In this study, new series of azetidine derivatives were synthesized (4a‐n) from isoniazide (1), Aromatic aldehydes (2a‐n), dihydropyran (3) using SnCl₂ catalyst, via one pot multicomponent reaction/cycloaddition reaction. The synthesized azetidine derivatives were characterized by IR, ¹H NMR and ¹³C NMR and have been screened for antimicrobial, antituberculosis and anti‐inflammatory activities. In relation to Staphylococcus aureus (ATCC 25923) promising antibacterial activity was shown, compounds 4e and 4k, followed by compounds 4h, 4n, 4f, 4g and 4l. The synthesized azetidine derivatives, 4a, 4e, 4j and 4m (with zone 12 mm) displayed antituberculosis activity. But its lower potential than, the standard streptomycin (with zone 18 mm). Further 4d compound alone displayed similar activity.

中文翻译：

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超声辅助合成N-（7-（R）-2-氧杂-8-氮杂双环[4.2.0]辛烷-8-基）异烟酰胺衍生物及其生物学评价

在这项研究中，通过一锅多组分反应/环加成反应，使用SnCl ₂催化剂从异烟肼（1），芳香醛（2a-n），二氢吡喃（3）合成了一系列新的氮杂环丁烷衍生物（4a-n）。合成的氮杂环丁烷衍生物通过IR，¹ H NMR和¹³ C NMR表征，并已筛选出抗微生物，抗结核和抗炎活性。对于金黄色葡萄球菌（ATCC 25923），显示了有希望的抗菌活性，化合物4e和4k，其次是化合物4h和4n，4f，4g和4l。合成的氮杂环丁烷衍生物4a，4e，4j和4m（区域为12 mm）显示出抗结核活性。但是它的潜力比标准链霉素（区域18 mm）低。单独的另外的4d化合物表现出相似的活性。