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Benzoxazole derivatives: design, synthesis and biological evaluation.
BMC Chemistry ( IF 4.3 ) Pub Date : 2018-08-14 , DOI: 10.1186/s13065-018-0459-5
Saloni Kakkar 1 , Sumit Tahlan 1 , Siong Meng Lim 2, 3 , Kalavathy Ramasamy 2, 3 , Vasudevan Mani 4 , Syed Adnan Ali Shah 2, 5 , Balasubramanian Narasimhan 1
Affiliation  

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.

中文翻译:

苯并恶唑衍生物:设计,合成和生物学评估。

背景技术合成了一系列新的苯并恶唑类似物,并检查了它们的体外抗菌,抗真菌和抗癌活性。结果与讨论合成的苯并恶唑化合物经IR,1H / 13C-NMR确证,并筛选了其对革兰氏阳性菌:枯草芽孢杆菌,四种革兰氏阴性菌:大肠杆菌,铜绿假单胞菌,肺炎克雷伯菌的体外抗菌活性。 ,伤寒沙门氏菌和两种真菌菌株:白色念珠菌和黑曲霉,采用管稀释技术,最小抑菌浓度(MIC)以µM表示,并与氧氟沙星和氟康唑进行比较。使用人类大肠癌(HCT116)癌细胞系,通过以5-氟尿嘧啶为标准药物的磺胺多巴胺B测定法测定体外抗癌活性(IC50值)。
更新日期:2019-11-01
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