Imidazo[4,5‐ b ]pyridine Derivatives of Potential Tuberculostatic Activity. Part 1: Synthesis and Quantitative Structure‐Activity Relationships | Zendy

Bukowski Ludwik | Zendy; Kaliszan Roman | Zendy

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Imidazo[4,5‐ b ]pyridine Derivatives of Potential Tuberculostatic Activity. Part 1: Synthesis and Quantitative Structure‐Activity Relationships

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.19913240212

Subject(s) - quantitative structure–activity relationship , chemistry , pyridine , stereochemistry , imidazole , mycobacterium tuberculosis , structure–activity relationship , biological activity , combinatorial chemistry , organic chemistry , biochemistry , in vitro , tuberculosis , medicine , pathology

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.

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