Design and microwave-assisted synthesis of a novel Mannich base and conazole derivatives and their biological assessment

IF 1.3 3区 化学 Q3 CHEMISTRY, ORGANIC Heterocyclic Communications Pub Date : 2021-01-01 DOI:10.1515/hc-2020-0126
Yıldız Uygun Cebeci, S. Karaoglu
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引用次数: 1

Abstract

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.
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新型曼尼奇碱和酮康唑衍生物的设计、微波合成及其生物学评价
摘要4-氨基-5-甲基-2,4-二氢-3H-1,2,4-三唑-3-酮(1)经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啉酮核的曼尼奇碱。此外,从1,2,4-三唑-3-酮化合物开始,通过常规或微波介导的条件,通过三个步骤合成了六种可被认为是酮康唑类似物的化合物。对所有新合成的化合物进行了抗菌活性筛选。大多数表现出良好至中度的抗菌和/或抗真菌活性。新化合物的结构归属是基于元素分析和光谱(IR,1H 核磁共振,13C NMR和LC-MS)数据。
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来源期刊
Heterocyclic Communications
Heterocyclic Communications 化学-有机化学
CiteScore
3.80
自引率
4.30%
发文量
13
审稿时长
1.4 months
期刊介绍: Heterocyclic Communications (HC) is a bimonthly, peer-reviewed journal publishing preliminary communications, research articles, and reviews on significant developments in all phases of heterocyclic chemistry, including general synthesis, natural products, computational analysis, considerable biological activity and inorganic ring systems. Clear presentation of experimental and computational data is strongly emphasized. Heterocyclic chemistry is a rapidly growing field. By some estimates original research papers in heterocyclic chemistry have increased to more than 60% of the current organic chemistry literature published. This explosive growth is even greater when considering heterocyclic research published in materials science, physical, biophysical, analytical, bioorganic, pharmaceutical, medicinal and natural products journals. There is a need, therefore, for a journal dedicated explicitly to heterocyclic chemistry and the properties of heterocyclic compounds.
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