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Design and microwave-assisted synthesis of a novel Mannich base and conazole derivatives and their biological assessment
Heterocyclic Communications ( IF 2.3 ) Pub Date : 2021-01-01 , DOI: 10.1515/hc-2020-0126
Yıldız Uygun Cebeci 1 , Şengül Alpay Karaoğlu 2
Affiliation  

Abstract 4-Amino-5-methyl-2,4-dihydro-3H-1,2,4-triazol-3-one (1) was converted to the corresponding Schiff base (2) by treatment with salicylaldehyde. 1,2,4-Triazoles were then converted to the corresponding Mannich bases containing fluroquinolone core using a one-pot three-component procedure. Moreover, the synthesis of six compounds, which can be considered as conazole analogues, was performed starting from 1,2,4-triazole-3-one compounds via three steps by either conventional or microwave-mediated conditions. All the newly synthesized compounds were screened for their antimicrobial activities. Most exhibited good to moderate antibacterial and/or antifungal activity. The structural assignments of the new compounds were based on elemental analysis and spectral (IR, 1H NMR, 13C NMR, and LC-MS) data.

中文翻译:

新型曼尼希碱和康唑衍生物的设计和微波辅助合成及其生物学评价

摘要 4-Amino-5-methyl-2,4-dihydro-3H-1,2,4-triazol-3-one (1) 通过水杨醛处理转化为相应的席夫碱 (2)。然后使用一锅三组分程序将1,2,4-三唑转化为相应的含有氟喹诺酮核心的曼尼希碱。此外,可以认为是康唑类似物的六种化合物的合成是从 1,2,4-triazole-3-one 化合物开始,通过常规或微波介导条件的三个步骤进行的。筛选所有新合成的化合物的抗菌活性。大多数表现出良好至中等的抗菌和/或抗真菌活性。新化合物的结构分配基于元素分析和光谱(IR、1H NMR、13C NMR 和 LC-MS)数据。
更新日期:2021-01-01
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