Department of Chemistry, Faculty of Science, Arish University, Arish, 45511, Egypt.
Mol Divers. 2022 Apr;26(2):741-755. doi: 10.1007/s11030-020-10152-9. Epub 2021 Jan 5.
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, H-NMR, C-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.
含萘环部分的化合物由于具有广泛的生物活性和低毒性,可作为药物制剂。在这项研究中,通过关键中间体 1-(1-羟基-2-萘基)-3-苯基-1,3-丙二酮 3 与各种亲电和亲核试剂在多种温和条件下反应,合成了一系列新的唑类或嗪类化合物。这些化合物的化学结构通过各种光谱方法(如(IR、H-NMR、C-NMR、质谱和元素分析)得到确认。合成的化合物在体外进行了抗微生物活性筛选,以测试它们对一些革兰氏阳性菌(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)的抑制作用。化合物的抗真菌活性也对酵母和丝状真菌(白色念珠菌和黄曲霉)进行了测试。该系列化合物的抗菌活性表现出较弱或中等的活性。