Department of Chemistry, Kakatiya University, Warangal 506 009, A.P., India.
Eur J Med Chem. 2012 Apr;50:344-9. doi: 10.1016/j.ejmech.2012.02.013. Epub 2012 Feb 13.
A series of novel methylene bis-isoxazolo[4,5-b]azepines have been synthesized by reaction of 3,5-dimethyl-4-nitroisoxazole 6 with an appropriate methylene bis-chalcones 7 to obtain various Michael adducts 8a-i, which on treatment with SnCl(2)-MeOH underwent reductive cyclization to afford the title compounds 9a-i. Structure of these compounds were established on the basis of IR, (1)H NMR, (13)C NMR and mass spectral data. The title compounds 9a-i were evaluated for their in vitro antimicrobial and anticancer activities. Compounds 9h and 9i exhibited potent antimicrobial and anticancer activities as that of standard drugs.
一系列新型亚甲基双异噁唑并[4,5-b]氮杂卓已通过 3,5-二甲基-4-硝基异噁唑 6 与适当的亚甲基双查尔酮 7 的反应合成，以获得各种迈克尔加成物 8a-i，其在 SnCl(2)-MeOH 处理下进行还原环化，得到标题化合物 9a-i。这些化合物的结构是基于 IR、(1)H NMR、(13)C NMR 和质谱数据建立的。对标题化合物 9a-i 进行了体外抗菌和抗癌活性评价。化合物 9h 和 9i 表现出与标准药物相当的强烈的抗菌和抗癌活性。
