Vinoth Kumar Sekar, Subramanian Mohan Raj, Chinnaiyan Santhosh Kumar
Department of Pharmaceutical Chemistry, Gokulakrishna College of Pharmacy, Andhra Pradesh 524121, India.
Department of Pharmacology, SSM College of Pharmacy, Tamil Nadu 638312, India.
J Young Pharm. 2013 Dec;5(4):154-9. doi: 10.1016/j.jyp.2013.11.004. Epub 2013 Dec 11.
Benzimidazoles and its derivatives represent one of the mainly biological active classes of literature.
In this present study aimed to synthesize N-mannich bases derivatives compounds bearing of 2-substituted benzimidazole moiety, in order to investigate their possible biological activity.
Benzimidazole compounds were prepared from the condensation reaction between ortho phenylene diamine and various acids. Mannich base of newly synthesized Benzimidazole derivatives were synthesized from 2-substituted Benzimidazoles by reacting with secondary amines. The purity of the compounds was ascertained by melting point (m.p) and thin layer chromatography (TLC). Structures of the synthesized compounds were elucidated by spectral data. Antimicrobial assay was performed by microbroth dilution method. Bacterial genomic DNA cleavage was assessed by Agarose gel electrophoresis. Toxicity of the most effective compounds was studied by Brine-shrimp lethality assay.
Among the synthesized compounds, compound 5E (a) and (b) was establish to be the most potent against all tested microorganisms. This two compounds exhibited complete bacterial DNA cleavage and non-toxic.
These results suggest that it an interesting compound compared to the current therapeutic agents and are considered to investigate further for the same.
苯并咪唑及其衍生物是文献中主要的生物活性类别之一。
在本研究中,旨在合成带有2-取代苯并咪唑部分的N-曼尼希碱衍生物化合物,以研究其可能的生物活性。
苯并咪唑化合物由邻苯二胺与各种酸之间的缩合反应制备。新合成的苯并咪唑衍生物的曼尼希碱通过与仲胺反应由2-取代苯并咪唑合成。化合物的纯度通过熔点(m.p)和薄层色谱法(TLC)确定。合成化合物的结构通过光谱数据阐明。抗菌试验通过微量肉汤稀释法进行。通过琼脂糖凝胶电泳评估细菌基因组DNA的切割。通过卤虫致死试验研究最有效化合物的毒性。
在合成的化合物中,化合物5E(a)和(b)被确定为对所有测试微生物最有效的。这两种化合物表现出完全的细菌DNA切割且无毒。
这些结果表明,与目前的治疗剂相比,它是一种有趣的化合物,并被认为需要进一步对此进行研究。