Rohini Rondla, Shanker Kanne, Reddy Puchakayala Muralidhar, Ho Yen-Peng, Ravinder Vadde
Department of Chemistry, Kakatiya University, Warangal, Andra Pradesh, India.
Eur J Med Chem. 2009 Aug;44(8):3330-9. doi: 10.1016/j.ejmech.2009.03.022. Epub 2009 Mar 27.
With the aim of obtaining novel biologically active compounds, we have synthesized a series of mono, bis-2-o-arylideneaminophenylbenzimidazoles and a second series of corresponding mono, bis-6-arylbenzimidazo[1,2-c]quinazolines respectively. The target benzimidazo[1,2-c]quinazoline compounds were obtained by the condensation of 2-(o-aminophenyl)benzimidazole with mono and di carbonyl compounds, followed by oxidative cyclisation of the resulting mono and bis-2-o-arylideneaminophenylbenzimidazoles.All the products were characterized via IR, (1)H NMR, (13)C NMR, MS and elemental analysis. The antimicrobial activities of all quinazolines against various bacteria and fungi were evaluated. Among the compounds tested IVd, IVe exhibited good antibacterial and antifungal activities while IIIb, IIIc also showed notable antimicrobial activity with reference to standard drugs Ampicillin and Ketoconazole respectively.
为了获得新型生物活性化合物，我们分别合成了一系列单、双-2-o-亚芳基氨基苯基苯并咪唑以及第二系列相应的单、双-6-芳基苯并咪唑并[1,2-c]喹唑啉。目标苯并咪唑并[1,2-c]喹唑啉化合物是通过2-(o-氨基苯基)苯并咪唑与单羰基和二羰基化合物缩合，然后将所得的单和双-2-o-亚芳基氨基苯基苯并咪唑进行氧化环化反应得到的。所有产物均通过红外光谱、(1)H核磁共振、(13)C核磁共振、质谱和元素分析进行了表征。评估了所有喹唑啉对各种细菌和真菌的抗菌活性。在所测试的化合物中，IVd、IVe表现出良好的抗菌和抗真菌活性，而IIIb、IIIc相对于标准药物氨苄青霉素和酮康唑也分别表现出显著的抗菌活性。
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