New polyfunctional imidazo[4,5-C]pyridine motifs: Synthesis, crystal studies, docking studies and antimicrobial evaluation

作者：Jose Gilish; Kumara T H Suresha^*; Nagendrappa Gopalpur; Sowmya H B V; Jasinski Jerry P; Millikan Sean P; Chandrika N; More Sunil S; Harish B G

来源：European Journal of Medicinal Chemistry, 2014, 77: 288-297.

DOI：10.1016/j.ejmech.2014.03.019

• Imidazo[4,5-c]pyridine
• Microwave-assisted organic synthesis
• X-ray crystal studies
• Antimicrobial activity
• Molecular docking studies

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, H-1 NMR, C-13 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 91 displayed promising antimicrobial activity. The molecular docking of GlcN-6-P synthase with newly synthesized compounds was carried out.

• 出版日期2014-4