کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
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1396584 | 1501196 | 2009 | 8 صفحه PDF | دانلود رایگان |
![عکس صفحه اول مقاله: Design, synthesis and antimycobacterial activity of some novel imidazo[1,2-c]pyrimidines Design, synthesis and antimycobacterial activity of some novel imidazo[1,2-c]pyrimidines](/preview/png/1396584.png)
Tuberculosis, due to its relentless nature, is now a major public health threat. The concomitant resurgence of TB with the MDR- or XDR-TB and HIV/AIDS pandemic has exposed the frailties of the current drug armatorium. Based on isosteric replacement and good 3D structural similarity between PA-824, a novel antimycobacterial agent undergoing clinical trials, and imidazo[1,2-c]pyrimidines, we have designed novel imidazo[1,2-c]pyrimidines. The designed molecules were synthesized by nucleophilic displacement of chloro group of various substituted 4-chloropyrimidines by ethanolamine followed by cyclisation of these 4-(2-hydroxyethyl)aminopyrimidines to imidazo[1,2-c]pyrimidines in good yield. All the compounds were screened for their antimycobacterial activity on Mycobacterium tuberculosis H37Rv strain by 1% proportion method. Some of the synthesized compounds exhibited potent antimycobacterial activity with MIC values in the range of 2–20 μg/mL.
Design, synthesis and antimycobacterial activity of some novel imidazo[1,2-c]pyrimidines have been described. Some of the synthesized compounds exhibited significant antimycobacterial activity with MIC values in the range of 2–20 μg/mL. Figure optionsDownload as PowerPoint slide
Journal: European Journal of Medicinal Chemistry - Volume 44, Issue 10, October 2009, Pages 3837–3844