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Bis-(imidazole/benzimidazole)-pyridine derivatives: synthesis, structure and antimycobacterial activity
Vasilichia Antoci1, Dumitrela Cucu1, Gheorghita Zbancioc1
1Faculty of Chemistry, Alexandru Ioan Cuza University of Iasi, 11 Carol I Bd, Iasi 700506, Romania.
Abstract:
Aim: Over the last decades, few significant achievements have been made in tuberculosis (TB) therapy. As a result, there is an urgent need for new anti-TB drugs. Results: Two new classes of bis-(imidazole/benzimidazole)-pyridine derivatives were designed, synthesized and evaluated for their antimycobacterial activity. Conclusion: The synthesis is efficient and straightforward, involving only two successive N-alkylations. The anti-TB assay reveal that our compounds have an excellent anti-TB activity against both replicating and nonreplicating Mtb, are not cytotoxic, exhibited a very good intracellular activity and are active against drug-resistant Mtb strains, some compounds have a bactericidal mechanism. The absorption, distribution, metabolism, excretion and toxicity studies performed for one compound are promising, indicating that it is a good candidate for a future drug.
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