Synthesis, in vitro Antibacterial and Cytotoxic studies of novel Naphthofurans

K. Mathiyazhagan, P. Arjun, S. Vennila
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Abstract

A simple, convenient and reproducible naphthofuran derivatives (1-5) were synthesized from 1,4-naphthoquinones and characterized by 1 H-NMR, 13 C-NMR, FT-IR, and Mass spectral studies. All the newly synthesized compounds were evaluated for in vitro antibacterial activity against Staphylococcus aureus (ATCC 6538) , Staphylococcus epidermidis (ATCC 155) and Bacillus cereus (ATCC 11778) as Gram positive bacteria; Escherichia coli (ATCC 25922) , Klebsiella pneumonia (ATCC 29665) and Pseudomonas aeruginosa (ATCC 25619) as Gram negative bacteria and their minimal inhibitory concentrations were determined. Amongst the tested organisms, compound 1 was the most active compound against all the tested organisms. All the compounds were evaluated for in vitro cytotoxicity potential using the standard MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) assay against  human cervical cancer cell line (HeLa) and compound 3 showed more  potent than other compounds.
新型萘呋喃的合成、体外抗菌及细胞毒性研究
以1,4-萘醌为原料合成了一种简单、方便、重现性好的萘呋喃衍生物(1-5),并通过1h - nmr、13c - nmr、FT-IR和质谱对其进行了表征。所有新合成的化合物对革兰氏阳性菌金黄色葡萄球菌(ATCC 6538)、表皮葡萄球菌(ATCC 155)和蜡样芽孢杆菌(ATCC 11778)的体外抗菌活性进行了评价;测定革兰氏阴性菌为大肠埃希菌(ATCC 25922)、肺炎克雷伯菌(ATCC 29665)和铜绿假单胞菌(ATCC 25619)及其最小抑菌浓度。化合物1对所有被试生物的活性最高。采用标准MTT(3-(4,5-二甲基噻唑-2-基)-2,5-二苯基溴化四唑)法评价了化合物对人宫颈癌细胞株(HeLa)的体外细胞毒性,结果表明化合物3的体外细胞毒性强于其他化合物。
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