Imidazo[4,5-b]pyridine derivatives of potential tuberculostatic activity. Part 1: Synthesis and quantitative structure-activity relationships.
New derivatives of imidazo[4,5-b]pyridine and 9H-dipyrido-[1,2-a:3',2'-d]imidazole were synthesized. Antibacterial activity against Mycobacterium tuberculosis of selected compounds was determined. These data were combined with the corresponding bioactivity data previously generated for two other series of imidazo[4,5-b]pyridines. Analysis of Quantitative Structure-Activity Relationships [QSAR] was carried out using nonempirical structural descriptors. Hydrophobicity of the agents studied was found decisive for their activity. A QSAR equation was derived allowing rational design of active derivatives.
Bukowski
L
L
Department of Organic Chemistry, Medical Academy, Gdansk, Poland.
Kaliszan
R
R
D000995:Antitubercular Agents / Q000138:chemical synthesis*; D008826:Microbial Sensitivity Tests; D009169:Mycobacterium tuberculosis / Q000187:drug effects; D011687:Purines / Q000138:chemical synthesis* / Q000494:pharmacology; D013329:Structure-Activity Relationship
D000995:Antitubercular Agents; D011687:Purines; C064191:1H-imidazo(4,5-b)pyridine