苯并恶唑衍生物：设计、合成及生物学评价

Benzoxazole derivatives: design, synthesis and biological evaluation.

作者信息

Kakkar Saloni, Tahlan Sumit, Lim Siong Meng, Ramasamy Kalavathy, Mani Vasudevan, Shah Syed Adnan Ali, Narasimhan Balasubramanian

机构信息

Faculty of Pharmaceutical Sciences, Maharshi Dayanand University, Rohtak, 124001, India.

Faculty of Pharmacy, Universiti Teknologi MARA (UiTM), Puncak Alam Campus, 42300, Bandar Puncak Alam, Selangor Darul Ehsan, Malaysia.

出版信息

Chem Cent J. 2018 Aug 12;12(1):92. doi: 10.1186/s13065-018-0459-5.

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, H/C-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 (IC 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.

背景

合成了一系列新的苯并恶唑类似物，并检测了它们的体外抗菌、抗真菌和抗癌活性。

结果与讨论

通过红外光谱（IR）、氢碳核磁共振（H/C-NMR）、质谱对合成的苯并恶唑化合物进行了确证，并采用试管稀释技术筛选了它们对革兰氏阳性菌枯草芽孢杆菌、四种革兰氏阴性菌大肠杆菌、铜绿假单胞菌、肺炎克雷伯菌、伤寒沙门氏菌以及两种真菌白色念珠菌和黑曲霉的体外抗菌活性，以微摩尔（µM）为单位记录最低抑菌浓度（MIC），并与氧氟沙星和氟康唑进行比较。使用人结肠癌细胞系（HCT116），以5-氟尿嘧啶为标准药物，通过磺基罗丹明B法测定体外抗癌活性（IC值）。