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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
Author(s) -
Bukowski Ludwik,
Kaliszan Roman
Publication year - 1991
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.2503240903
Subject(s) - pyridine , chemistry , quantitative structure–activity relationship , mycobacterium tuberculosis , antibacterial activity , stereochemistry , biological activity , in vitro , medicinal chemistry , tuberculosis , biochemistry , bacteria , biology , medicine , pathology , genetics
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‐4 H ‐2‐cyanomethylimidazo[4,5‐ b ]pyridine (7) and 2‐(α‐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.