Jose Gilish, Suresha Kumara T H, Nagendrappa Gopalpur, Sowmya H B V, Jasinski Jerry P, Millikan Sean P, Chandrika N, More Sunil S, Harish B G
P.G. Department of Chemistry, Jain University, 127/2, Bull Temple Road, Chamarajpet, Bangalore 560026, India.
P.G. Department of Chemistry, Jain University, 127/2, Bull Temple Road, Chamarajpet, Bangalore 560026, India; Department of Chemistry, U.B.D.T. College of Engineering, Davangere, Karnataka 577004, India.
Eur J Med Chem. 2014 Apr 22;77:288-97. doi: 10.1016/j.ejmech.2014.03.019. Epub 2014 Mar 11.
New antimicrobial agents, imidazo[4,5-c]pyridine derivatives have been synthesized. We have developed a new synthetic protocol for the final reaction, an efficient microwave-assisted synthesis of imidazo[4,5-c]pyridines from substituted 3,4-diaminopyridine and carboxylic acids in presence of DBU mediated by T3P. The chemical structures of the new compounds were characterized by IR, (1)H NMR, (13)C NMR, mass spectral analysis and elemental analysis. In addition, single crystal X-ray diffraction has also been recorded for compound 9c. The in vitro antimicrobial activities of the compounds were conducted against various Gram-negative, Gram-positive bacteria and fungi. Amongst the tested compounds 9c, 9e, 9g, 9k and 9l displayed promising antimicrobial activity. The molecular docking of GlcN-6-P synthase with newly synthesized compounds was carried out.
新型抗菌剂咪唑并[4,5-c]吡啶衍生物已被合成。我们开发了一种用于最终反应的新合成方法,即由T3P介导,在DBU存在下,通过微波辅助从取代的3,4-二氨基吡啶和羧酸高效合成咪唑并[4,5-c]吡啶。通过红外光谱、核磁共振氢谱、核磁共振碳谱、质谱分析和元素分析对新化合物的化学结构进行了表征。此外,还对化合物9c进行了单晶X射线衍射分析。对这些化合物进行了针对各种革兰氏阴性菌、革兰氏阳性菌和真菌的体外抗菌活性测试。在测试的化合物中,9c、9e、9g、9k和9l表现出有前景的抗菌活性。还对新合成的化合物进行了葡糖胺-6-磷酸合酶的分子对接研究。