Imidazo[4,5‐b]pyridine derivatives of potential tuberculostatic activity, II: Synthesis and bioactivity of designed and some other 2‐cyanomethylimidazo[4,5‐b]pyridine derivatives

Based on the analysis of Quantitative Structure--Activity Relationships (QSAR) three representatives of imidazo[4,5-b]pyridine derivatives of predicted high antibacterial activity against Mycobacterium tuberculosis were synthetized and tested bacteriologically. Excellent agreement of the predicted and experimentally observed bioactivity was noted. Additional new derivatives of 4-methyl-4H-2-cyanomethylimidazo[4,5-b]pyridine (7) and 2-(alpha-methylcyanomethyl)imidazo[4,5-b]pyridine (22) were also synthesized and some of them were tested for tuberculostatic activity. The compounds synthesized according to a standard "trial and error" approach appeared generally inactive.