Bis-(imidazole/benzimidazole)-pyridine derivatives: Synthesis, structure and antimycobacterial activity
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ANTOCI, Vasilichia, CUCU, Dumitrela, ZBANCIOC, Gheorghita N., MOLDOVEANU, Costel, MANGALAGIU, Violeta, AMĂRIUCĂI-MANTU, Dorina, ARICU, Aculina, MANGALAGIU, Ionel. Bis-(imidazole/benzimidazole)-pyridine derivatives: Synthesis, structure and antimycobacterial activity. In: Future Medicinal Chemistry, 2020, nr. 3(12), pp. 207-222. ISSN 1756-8919. DOI: 10.4155/fmc-2019-0063
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Future Medicinal Chemistry
Numărul 3(12) / 2020 / ISSN 1756-8919 /ISSNe 1756-8927

Bis-(imidazole/benzimidazole)-pyridine derivatives: Synthesis, structure and antimycobacterial activity


Pag. 207-222

Antoci Vasilichia1, Cucu Dumitrela1, Zbancioc Gheorghita N.1, Moldoveanu Costel1, Mangalagiu Violeta21, Amăriucăi-Mantu Dorina1, Aricu Aculina3, Mangalagiu Ionel1
1 Alexandru Ioan Cuza University of Iaşi,
2 Institute of Interdisciplinary Research – CERNESIM Centre,
3 Institute of Chemistry

Noi substanțe cu potențial preventiv și terapeutic în baza compușilor naturali de origine vegetală și a matodelor moderne de sinteză organică

Disponibil în IBN: 6 martie 2020


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.

ADMET, antimycobacterial, bis-(imidazole/benzimidazole)-pyridine, MBC, MIC