Synthesis, Characterization and Biological Screening of Azepine Derivative: 2-hydroxy-1,3-di(naphthalene-2-yl)-1H-benzo[b]azepine-5(4H)one

A. Sharma, Ashok K. Singh
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Abstract

The synthesis of unsaturated heterocyclic compounds containing nitrogen atoms in the ring is very important due to its various biological application in the pharmaceutical industry. Azepine derivatives find numerous application almost every field in medicinal chemistry and some of its are commercially available as drugs. The two-component of azepine derivatives were synthesized by using the aniline and maleic anhydride as a starting material followed by condensation with sodium borohydride in presence of dry benzene, subsequently cyclization by polyphosphoric acid then, finally by an addition reaction with naphthalene-2-ol to form the desired derivative. The formation of the synthesized azepine derivative was confirmed by spectral techniques such as IR, 1H-NMR, and 13C-NMR. The antibacterial assay shows that the synthesized compound (2A) possesses the most highly potent activity in the Bacillus subtilis and moderate activity against other different strains of bacteria and fungi.
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氮平衍生物:2-羟基-1,3-二(萘-2-基)- 1h -苯并[b]氮平-5(4H) 1的合成、表征及生物学筛选
含氮不饱和杂环化合物的合成由于其在制药工业中的各种生物应用而具有十分重要的意义。氮卓类衍生物几乎在药物化学的每个领域都有广泛的应用,其中一些是商业上可用的药物。以苯胺和马来酸酐为原料,在干苯存在下与硼氢化钠缩合,再经多磷酸环化,最后与萘-2-醇加成,合成双组分氮平衍生物。通过IR、1H-NMR和13C-NMR等光谱技术证实了合成的氮卓类衍生物的形成。抑菌实验表明,合成的化合物(2A)对枯草芽孢杆菌具有最强的抑菌活性,对其他不同菌株的细菌和真菌具有中等的抑菌活性。
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