【摘 要】
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Pyrimidines have gained great therapeutic importance in the field of medicinal chemistry due to their extensively biological activities.Especially in antimicrobial aspects,many pyrimidines such as sul
【机 构】
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Institute of Bioorganic & Medicinal Chemistry, School of Chemistry and Chemical Engineering, Southwe
【出 处】
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中国化学会第十三届全国有机合成化学学术研讨会
论文部分内容阅读
Pyrimidines have gained great therapeutic importance in the field of medicinal chemistry due to their extensively biological activities.Especially in antimicrobial aspects,many pyrimidines such as sulfadiazine and voriconazole have been in widespread clinical use to treat diseases caused by bacteria and fungi.Such fragments have been prevalently employed in the design of new drugs.Herein we developed a series of novel aminopyrimidine-based benzimidazoles with halogen substituents and different lengths of aliphatic chains.The target compounds were obtained starting from o-phenylene diamines via multistep reactions and further confirmed by NMR,MS and IR spectra.The biological assay manifested that compound 3g showed comparable or even better antibacterial activities than reference drugs.Its anti-MRSA efficacy (MIC =2 μg/mL) was 8-fold more potent than Chloromycin.
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