Benzoxazole derivatives: design, synthesis and biological evaluation.

Q1 Chemistry Chemistry Central Journal Pub Date : 2018-08-12 DOI:10.1186/s13065-018-0459-5
Saloni Kakkar, Sumit Tahlan, Siong Meng Lim, Kalavathy Ramasamy, Vasudevan Mani, Syed Adnan Ali Shah, Balasubramanian Narasimhan
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引用次数: 47

Abstract

Background: A new series of benzoxazole analogues was synthesized and checked for their in vitro antibacterial, antifungal and anticancer activities.

Results and discussion: The synthesized benzoxazole compounds were confirmed by IR, 1H/13C-NMR, mass and screened for their in vitro antimicrobial activity against Gram-positive bacterium: Bacillus subtilis, four Gram-negative bacteria: Escherichia coli, Pseudomonas aeruginosa, Klebsiella pneumoniae, Salmonella typhi and two fungal strains: Candida albicans and Aspergillus niger using tube dilution technique and minimum inhibitory concentration (MIC) was noted in µM and compared to ofloxacin and fluconazole. Human colorectal carcinoma (HCT116) cancer cell line was used for the determination of in vitro anticancer activity (IC50 value) by Sulforhodamine B assay using 5-fluorouracil as standard drug.

Conclusion: The performed study indicated that the compounds 1, 10, 13, 16, 19, 20 and 24 had highest antimicrobial activity with MIC values comparable to ofloxacin and fluconazole and compounds 4, 6, 25 and 26 had best anticancer activity in comparison to 5-fluorouracil.

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苯并恶唑衍生物:设计、合成及生物学评价。
背景:合成了一系列新的苯并恶唑类似物,并对其体外抗菌、抗真菌和抗癌活性进行了研究。结果与讨论:合成的苯并恶唑化合物经IR、1H/13C-NMR、质量鉴定,对革兰氏阳性菌枯草芽孢杆菌、4种革兰氏阴性菌大肠埃希菌、铜绿假单胞菌、肺炎克雷伯菌、伤寒沙门菌和2种真菌进行了体外抑菌活性筛选。用试管稀释法测定白色念珠菌和黑曲霉在µM内的最低抑菌浓度(MIC),并与氧氟沙星和氟康唑进行比较。以人大肠癌(HCT116)细胞株为研究对象,以5-氟尿嘧啶为标准药,采用硫代丹明B法测定其体外抗癌活性(IC50值)。结论:化合物1、10、13、16、19、20和24的抑菌活性最高,其MIC值与氧氟沙星和氟康唑相当,化合物4、6、25和26的抑菌活性与5-氟尿嘧啶相比最好。
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来源期刊
Chemistry Central Journal
Chemistry Central Journal 化学-化学综合
CiteScore
4.40
自引率
0.00%
发文量
0
审稿时长
3.5 months
期刊介绍: BMC Chemistry is an open access, peer reviewed journal that considers all articles in the broad field of chemistry, including research on fundamental concepts, new developments and the application of chemical sciences to broad range of research fields, industry, and other disciplines. It provides an inclusive platform for the dissemination and discussion of chemistry to aid the advancement of all areas of research. Sections: -Analytical Chemistry -Organic Chemistry -Environmental and Energy Chemistry -Agricultural and Food Chemistry -Inorganic Chemistry -Medicinal Chemistry -Physical Chemistry -Materials and Macromolecular Chemistry -Green and Sustainable Chemistry
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