Department of Chemistry, University of Delhi, Delhi 110 007, India.
Eur J Med Chem. 2010 Apr;45(4):1502-7. doi: 10.1016/j.ejmech.2009.12.058. Epub 2010 Jan 13.
A series of 3,4-dihydro-2H-benzo[e]-, 2,3-dihydro-1H-naphtho[1,2-e]-, 3,4-dihydro-2H-naphtho[2,1-e][1,3]oxazine and 1,2-bis(3,4-dihydrobenzo[e][1,3]oxazin-3(4H)-yl)ethane derivatives was obtained through an eco-friendly Mannich type condensation-cyclization reaction of phenols or naphthols with formaldehyde and primary amines in water at ambient temperature. Preliminary in vitro antimicrobial activity of the synthesized compounds was assessed against six pathogenic fungi, two Gram-negative and two Gram-positive bacteria. Some of the screened compounds have shown significant in vitro antimicrobial effect. Cytotoxic activities of the lead compounds (2m, 2n, 3c and 3d) against mouse fibroblast cell line (L929) were determined by MTT method. The assay results revealed that these molecules offered remarkable viability (>90%) of L929 cells at concentration of 25 microg/mL.
通过酚类或萘酚与甲醛和伯胺在水介质中于环境温度下的绿色曼尼希型缩合-环化反应，得到了一系列 3,4-二氢-2H-苯并[e]-, 2,3-二氢-1H-萘并[1,2-e]-, 3,4-二氢-2H-萘并[2,1-e][1,3]恶嗪和 1,2-双(3,4-二氢苯并[e][1,3]恶嗪-3(4H)-基)乙烷衍生物。初步的体外抗微生物活性评估表明，所合成的化合物对六种致病真菌、两种革兰氏阴性菌和两种革兰氏阳性菌具有显著的体外抗菌作用。一些筛选出的化合物表现出显著的体外抗微生物活性。通过 MTT 法测定了先导化合物（2m、2n、3c 和 3d）对小鼠成纤维细胞系（L929）的细胞毒性。结果表明，这些分子在 25μg/mL 的浓度下对 L929 细胞具有显著的活力（>90%）。
