Puthran Divyaraj, Poojary Boja, Purushotham Nikil, Harikrishna Nandam, Nayak Soukhyarani Gopal, Kamat Vinuta
Department of Studies in Chemistry, Mangalore University, Mangalagangothri, Karnataka, 574199, India.
Solara Active Pharma Sciences, No. 120 A&B, Industrial Area, Baikampady, New Mangalore, Karnataka, 575011, India.
Heliyon. 2019 Aug 26;5(8):e02233. doi: 10.1016/j.heliyon.2019.e02233. eCollection 2019 Aug.
2-Amino-5-(3-fluoro-4-methoxyphenyl)thiophene-3-carbonitrile have been synthesized from 1-(3-fluoro-4-methoxyphenyl)ethanone, malononitrile, a mild base and sulfur powder using Gewald synthesis technique and the intermediate was treated with 1,3-disubstituted pyrazole-4-carboxaldehyde to obtain the novel Schiff bases. 1,3-disubstituted pyrazole-4-carboxaldehyde derivatives have been synthesized by Vilsmeier-Haack reaction in the course of a multi-step reaction. The structure of novel compounds were established on the basis of their elemental analyses IR, H NMR, C NMR, and mass spectral data and then screened for their antimicrobial activity. Among them 5a, 5c, 5f and 5h showed excellent activity when compared to other derivatives. Remaining derivatives showed moderate activity.
使用格瓦尔德合成技术，由1-（3-氟-4-甲氧基苯基）乙酮、丙二腈、一种温和的碱和硫粉合成了2-氨基-5-（3-氟-4-甲氧基苯基）噻吩-3-腈，然后将中间体与1,3-二取代吡唑-4-甲醛反应，得到新型席夫碱。1,3-二取代吡唑-4-甲醛衍生物是通过多步反应中的维尔斯迈尔-哈克反应合成的。根据元素分析、红外光谱、氢核磁共振谱、碳核磁共振谱和质谱数据确定了新型化合物的结构，然后对其抗菌活性进行了筛选。其中5a、5c、5f和5h与其他衍生物相比表现出优异的活性。其余衍生物表现出中等活性。
