Abstract

The compounds bearing naphthalene moiety can be used as medical preparations because of their wide spectrum of biological activity and low toxicity. In this study, a new series of azoles or azines were synthesized from the reaction of the key intermediate 1-(1-hydroxynaphthalen-2-yl)-3-phenylpropane-1,3-dione 3 with a variety of electrophilic and nucleophilic reagents under a variety of mild conditions. The chemical structures of these compounds were confirmed by various spectroscopic methods such as (IR, ¹H-NMR, ¹³C-NMR, mass spectra and elemental analyses). The prepared compounds were screened in vitro for their anti-microbial activity against some species of Gram-positive bacteria (Staphylococcus aureus and Bacillus subtilis) and Gram-negative bacteria (Escherichia coli and Pseudomonas aeuroginosa). Anti-fungal activities of the compounds were tested against yeast and mycelial fungi,Candida albicans and Aspergillus flavus. The antimicrobial activity of this series was showed either weak or moderate activities.

Graphic abstract

中文翻译：

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微波辅助 1,3-二酮的短时间清洁合成作为杂环合成中的构件：新型二氢吡啶、4H-吡喃、二氢哒嗪、嘧啶和吡唑衍生物的简便合成和抗菌评估

摘要

具有萘部分的化合物具有广泛的生物活性和低毒性，可用作医药制剂。在这项研究中，由关键中间体 1-(1-hydroxynaphthalen-2-yl)-3-phenylpropane-1,3-dione 3与多种亲电和亲核试剂反应合成了一系列新的唑类或吖嗪类。在各种温和条件下。这些化合物的化学结构通过各种光谱方法如（IR、¹ H-NMR、¹³ C-NMR、质谱和元素分析）证实。在体外筛选制备的化合物对某些革兰氏阳性细菌（金黄色葡萄球菌和枯草芽孢杆菌）和革兰氏阴性菌（大肠杆菌和铜绿假单胞菌）。测试了化合物对酵母和菌丝体真菌、白色念珠菌和黄曲霉的抗真菌活性。该系列的抗菌活性表现为弱或中等活性。

图形摘要