2-巯基苯并咪唑席夫碱：设计、合成、抗菌研究及对 HCT-116 细胞系的抗癌活性。
2-Mercaptobenzimidazole Schiff Bases: Design, Synthesis, Antimicrobial Studies and Anticancer Activity on HCT-116 Cell Line.
机构信息
Faculty of Pharmaceutical Sciences, Maharshi Dayanand University, Rohtak-124001, India.
Faculty of Pharmacy, Universiti Teknologi MARA (UiTM), 42300 Bandar Puncak Alam, Selangor Darul Ehsan, Malaysia.
出版信息
Mini Rev Med Chem. 2019;19(13):1080-1092. doi: 10.2174/1389557518666181009151008.
BACKGROUND
Increased rate of mortality due to the development of resistance to currently available antimicrobial and anticancer agents initiated the need to develop new chemical entities for the treatment of microbial infections and cancer.
OBJECTIVE
The present study was aimed to synthesize and evaluate antimicrobial and anticancer activities of Schiff bases of 2-mercaptobenzimidazole.
METHODS
The Schiff bases of 2-mercaptobenzimidazole were synthesized from 4-(2-(1H-benzo[d]- imidazol-2-ylthio)acetamido)benzohydrazide. The synthesized compounds were evaluated for antimicrobial and anticancer activities by tube dilution method and Sulforhodamine-B (SRB) assay, respectively.
RESULTS
Compounds 8 (MICpa, an = 2.41, 1.20 µM/ml), 10 (MICse, sa = 2.50 µM/ml), 20 (MICec = 2.34 µM/ml) and 25 (MICca = 1.46 µM/ml) showed significant antimicrobial activity against tested bacterial and fungal strains and compounds 20 (IC50 = 8 µg/ml) and 23 (IC50 = 7 µg/ml) exhibited significant anticancer activity.
CONCLUSION
In general, the synthesized derivatives exhibited moderate antimicrobial and anticancer activities. Compounds 8 and 25 having high antifungal potential among the synthesized compounds may be taken as lead molecules for the development of novel antifungal agents.
背景
由于现有抗菌和抗癌药物的耐药性发展导致死亡率增加，因此需要开发新的化学实体来治疗微生物感染和癌症。
目的
本研究旨在合成并评估 2-巯基苯并咪唑席夫碱的抗菌和抗癌活性。
方法
从 4-（2-（1H-苯并[d]-咪唑-2-基硫代）乙酰胺基）苯甲酰肼合成 2-巯基苯并咪唑席夫碱。通过管稀释法和磺基罗丹明 B（SRB）测定法分别评估合成化合物的抗菌和抗癌活性。
结果
化合物 8（MICpa，an = 2.41、1.20 µM/ml）、10（MICse，sa = 2.50 µM/ml）、20（MICec = 2.34 µM/ml）和 25（MICca = 1.46 µM/ml）对测试的细菌和真菌菌株表现出显著的抗菌活性，化合物 20（IC50 = 8 µg/ml）和 23（IC50 = 7 µg/ml）表现出显著的抗癌活性。
结论
总的来说，合成的衍生物表现出中等的抗菌和抗癌活性。在合成的化合物中，具有高抗真菌潜力的化合物 8 和 25 可能被视为开发新型抗真菌剂的先导化合物。
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