engleski

Biological activity of amidino-substituted imidazo [4,5-b]pyridines

A series of cyano and amidino substituted imidazo[4, 5-b]pyridines were synthesized using standard methods of organic synthesis and their biological activity was evaluated. Biological evaluation included in vitro antiproliferative effect on a diverse selection of human cancer cell lines, antibacterial activity against chosen Gram- positive and Gram-negative bacterial strains, and antiviral activity on a broad panel of DNA and RNA viruses. The most pronounced antiproliferative activity was observed for compound 10, with an unsubstituted amidino group, and compound 14, with a 2-imidazolinyl amidino group, both displaying selective and strong activity in sub micromolar inhibitory concentration range against colon carcinoma (IC50 0.4 and 0.7 μM, respectively). All tested compounds lacked antibacterial activity with exception of compound 14 which showed moderate activity against E. coli (MIC 32 μM). Bromo substituted derivative 7 with an unsubstituted phenyl ring (EC50 21 μM) and para- cyano substituted derivative 17 (EC50 58 μM) showed selective but moderate activity against Respiratory Syncytial Virus (RSV).

amidines; antibacterial activity; antiproliferative activity; antiviral activity; imidazo[4, 5-b]pyridines

KU Leuven, Department of Microbiology, Immunology and Transplantation, Laboratory of Virology and Chemotherapy, Rega Institute