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1,2,3-Triazole fused with pyridine/pyrimidine as new template for antimicrobial agents: Regioselective synthesis and identification of potent N-heteroarenes
Bioorganic & Medicinal Chemistry Letters ( IF 2.5 ) Pub Date : 2018-09-17 , DOI: 10.1016/j.bmcl.2018.09.021
Nagaraju Marepu , Sunandamma Yeturu , Manojit Pal

The 1,2,3-triazole ring fused with pyridine/pyrimidine was explored as new template for the identification of potential antimicrobial agents. The regioselective synthesis of these pre-designed N-heteroarenes was achieved via exploring the application of Buchwald’s strategy (i.e. C–N bond formation/reduction/diazotization/cyclization sequence) to the N-heteroarene system. Two of them showed promising antibacterial (comparable to streptomycin) and several showed potent antifungal (comparable to mancozeb) activities.



中文翻译:

1,2,3-三唑与吡啶/嘧啶融合作为抗菌剂的新模板:区域选择性合成和强力N-杂芳烃的鉴定

探索与吡啶/嘧啶稠合的1,2,3-三唑环作为鉴定潜在抗菌剂的新模板。这些预先设计的N-杂芳烃的区域选择性合成是通过探索将Buchwald策略(即C–N键形成/还原/重氮化/环化顺序)应用于N-杂芳烃体系而实现的。它们中的两个显示出有希望的抗菌作用(与链霉素相当),另外几个显示出有效的抗真菌作用(与mancozeb相当)。

更新日期:2018-09-17
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