Department of Chemistry, College of Science, King Saud University, PO Box 2455, Riyadh 11451, Saudi Arabia.
Bioorg Med Chem Lett. 2012 Feb 1;22(3):1375-9. doi: 10.1016/j.bmcl.2011.12.061. Epub 2011 Dec 20.
A facile and efficient synthesis of novel chromeno[4,3-b]pyrroles has been accomplished by intramolecular 1,3-dipolar cycloaddition which on subsequent Pictet-Spengler cyclisation in presence of p-toluenesulfonic acid yielded indolizino[6,7-b]indoles. The synthesized chromenopyrroles and indolizinoindoles were evaluated for their antimicrobial and antioxidant activities. Compounds 7b, 7e, 7a and 7d exhibited respectively, good antibacterial and antifungal activities against tested pathogens when compared to reference control.
通过分子内 1,3-偶极环加成反应,我们成功地实现了新型色烯并[4,3-b]吡咯的简便高效合成,随后在对甲苯磺酸存在下进行Pictet-Spengler 环化反应,得到了吲哚并[6,7-b]吲哚。我们对合成的色烯吡咯和吲哚并吲哚进行了抗菌和抗氧化活性评估。与对照品相比,化合物 7b、7e、7a 和 7d 分别表现出良好的抗细菌和抗真菌活性。