Department of Chemistry, Guru Jambheshwar University of Science & Technology, Hisar 125001, Haryana, India.
Eur J Med Chem. 2012 Oct;56:195-202. doi: 10.1016/j.ejmech.2012.08.018. Epub 2012 Aug 23.
A series of new 1,3-disubstituted-1H-naphtho[1,2-e][1,3]oxazines (3 and 7) was synthesized in good yields and the structure was determined with the help of NMR, 2D-NMR, HRMS studies and X-ray crystallography. These compounds were tested in vitro for their antibacterial activity against Gram-positive and Gram-negative bacteria and as well as for antifungal activity. The compounds 3c, 3e, 7a, 7d and 7k showed significant antibacterial activity and 7l showed moderate antifungal activity. The cytotoxicity of 1,3-disubstituted-1H-naphtho[1,2-e][1,3]oxazines showed that 3e and 7e are more effective against breast, lung and colon cell proliferation.
一系列新的 1,3-二取代-1H-萘并[1,2-e][1,3]恶嗪(3 和 7)以良好的产率合成,并通过 NMR、2D-NMR、HRMS 研究和 X 射线晶体学确定了其结构。这些化合物在体外进行了抗菌活性测试,包括对革兰氏阳性菌和革兰氏阴性菌的抗菌活性以及抗真菌活性。化合物 3c、3e、7a、7d 和 7k 表现出显著的抗菌活性,而 7l 则表现出中等的抗真菌活性。1,3-二取代-1H-萘并[1,2-e][1,3]恶嗪的细胞毒性表明,3e 和 7e 对乳腺癌、肺癌和结肠癌细胞的增殖更有效。