Isatin衍生物席夫碱高效合成的绿色化学方法及其抗菌活性评价

J. Panda, V. Patro, B. Sahoo, Jitendriya Mishra
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引用次数: 13

摘要

微波辅助有机合成作为一种绿色化学方法,在药物合成中得到了广泛的应用。微波辅助合成提高了药物化学家的吞吐量和周转时间,提供了大幅度减少反应时间,提高产量和产品纯度的好处。席夫碱是一类重要的有机化合物,由于其柔韧性和结构的多样性,由于存在亚甲基,这有助于阐明生物系统中转化和再散发反应的机理。这种新型化合物还可以作为有价值的配体,用于开发新的化学实体。本文采用微波加热的方法合成了一些Isatin衍生物的希夫碱。以鸢尾素的酮基与不同的芳香伯胺缩合为原料合成鸢尾素的希夫碱。利用光谱数据对它们进行了表征,并对革兰氏阳性和革兰氏阴性菌株进行了体外抗菌活性研究。结果表明,含吸电子取代基的化合物对几乎所有微生物都具有良好的抗菌活性。
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Green Chemistry Approach for Efficient Synthesis of Schiff Bases of Isatin Derivatives and Evaluation of Their Antibacterial Activities
Microwave-assisted organic synthesis, a green chemistry approach, is nowadays widely used in the drug synthesis. Microwave-assisted synthesis improves both throughput and turnaround time for medicinal chemists by offering the benefits of drastically reduced reaction times, increased yields, and pure products. Schiff bases are the important class of organic compounds due to their flexibility, and structural diversities due to the presence of azomethine group which is helpful for elucidating the mechanism of transformation and rasemination reaction in biological system. This novel compound could also act as valuable ligands for the development of new chemical entities. In the present work, some Schiff bases of Isatin derivatives was synthesized using microwave heating method. Schiff base of Isatin were synthesized by condensation of the keto group of Isatin with different aromatic primary amines. They were characterized by means of spectral data and subsequently subjected to the in vitro antibacterial activities against gram positive and gram negative strains of microbes. It was observed that the compound with electron withdrawing substituents exhibited good antibacterial activities against almost all the micro organisms.
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