新型噻吩[2,3-d]-嘧啶-4(3H)- 1衍生物的合成及抗菌活性研究

D. Kawade, A. Hadke
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引用次数: 0

摘要

疼痛和炎症是细菌感染的同时反应。在目前的临床实践中,抗菌药物等药物是同时使用的。以不同脂肪酸为原料,在常规加热和微波辐射下,POCl3催化高效一步无溶剂合成了2-氨基-4,5-取代噻吩-3-碳腈的新型噻吩[2,3 -d]嘧啶-4(3H)- 1衍生物。化合物的形成是通过元素分析和光谱技术,如FTIR, 1H NMR和质谱来证实的。所有合成的化合物对大肠杆菌(革兰氏菌)、枯草芽孢杆菌(革兰氏菌)的抑菌活性以及对黑曲霉和白色念珠菌的抑菌活性进行了筛选。结果表明,合成的化合物具有弱、中、好的抗菌活性。结果表明,化合物2a、2c、2d、2e、2f、2g、2j和2k具有较好的抑菌活性,其中化合物2b、2i、2j分别与标准药物Streptomycin和Amphotericin B相比具有显著的抑菌活性。关键词:POCl3, Thieno[2,3 -d]嘧啶-4 (3H)- 1,抗菌活性,链霉素,两性霉素B
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Synthesis and antimicrobial activities of some novel thieno [2,3-d]- Pyrimidin-4(3H)-One derivatives
Pain and inflammation are simultaneous responses in bacterial infections. In current clinical practice, the agents like antimicrobial drug are prescribed concurrently. A POCl3 catalyzed, efficient, one-step and solvent-free synthesis of novel thieno [2, 3-d] pyrimidin-4(3H)-one derivatives from 2-amino-4,5-substitutedthiophene-3-carbonitrile has been developed using various aliphatic acid under conventional heating and microwave irradiation. The formation of compounds was confirmed using elemental analysis and spectroscopic techniques like FTIR, 1H NMR and Mass spectroscopy. All synthesized compounds have been screened for their antimicrobial activity against Escherichia coli (Gram –ve strain), Bacillus subtilis (Gram +ve strain) for antibacterial activity and antifungal activities against Aspergillus niger and Candida albicans. The result showed that synthesized compounds exhibit weak, moderate and good antimicrobial activity. It was observed that the compounds 2a, 2c, 2d, 2e, 2f, 2g, 2j and 2k showed good antimicrobial activity whereas compounds 2b, 2i, 2j showed significant antimicrobial activity compared with standard drug Streptomycin and Amphotericin B respectively. Keyword:POCl3, Thieno[2, 3-d]pyrimidin-4 (3H)-one, Antimicrobial activity, Streptomycin and Amphotericin B
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