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以1,2,3-三唑并吡啶/嘧啶为新型抗菌剂模板:区域选择性合成及高效氮杂芳烃的鉴定

1,2,3-Triazole fused with pyridine/pyrimidine as new template for antimicrobial agents: Regioselective synthesis and identification of potent N-heteroarenes.

作者信息

Marepu Nagaraju, Yeturu Sunandamma, Pal Manojit

机构信息

Department of Chemistry, Acharya Nagarjuna University, Nagarjunanagar, Guntur 522510, Andhra Pradesh, India.

Department of Chemistry, Acharya Nagarjuna University, Nagarjunanagar, Guntur 522510, Andhra Pradesh, India.

出版信息

Bioorg Med Chem Lett. 2018 Nov 1;28(20):3302-3306. doi: 10.1016/j.bmcl.2018.09.021. Epub 2018 Sep 17.

Abstract

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.

摘要

将与吡啶/嘧啶稠合的1,2,3 - 三唑环作为鉴定潜在抗菌剂的新模板进行了探索。通过研究Buchwald策略(即C-N键形成/还原/重氮化/环化序列)在氮杂芳烃体系中的应用,实现了这些预先设计的氮杂芳烃的区域选择性合成。其中两种表现出有前景的抗菌活性(与链霉素相当),还有几种表现出强效的抗真菌活性(与代森锰锌相当)。

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