Bis-(imidazole/benzimidazole)-pyridine derivatives: synthesis, structure and antimycobacterial activity / Vasilichia Antoci, Dumitrela Cucu, Gheorghita Zbancioc, Costel Moldoveanu, Violeta Mangalagiu, Dorina Amariucai-Mantu, Aculina Aricu, Ionel I Mangalagiu
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 ofbis-(imidazole/benzimidazole)-pyridine derivatives were designed, synthesized and evaluated for their antimycobacterial activity.Conclusion:The synthesis is efficient and straightforward, involving only two successiveN-alkylations. The anti-TB assay reveal that our compounds have an excellent anti-TB activity against both replicating and nonreplicatingMtb, are not cytotoxic, exhibited a very good intracellular activity and are active against drug-resistantMtbstrains, 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. Aim: Results: bis Conclusion: N Mtb Mtb.
| Medienart: |
E-Artikel |
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| Erscheinungsjahr: |
2020 |
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| Erschienen: |
2020 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:12 |
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| Enthalten in: |
Future medicinal chemistry - 12(2020), 3, Seite 207- |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Antoci, Vasilichia [VerfasserIn] |
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| Links: |
FID Access [lizenzpflichtig] |
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| Umfang: |
1 Online-Ressource (16 p) |
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| doi: |
10.4155/fmc-2019-0063 |
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| funding: |
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| Förderinstitution / Projekttitel: |
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KFL001070371 |
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| 520 | |a 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 ofbis-(imidazole/benzimidazole)-pyridine derivatives were designed, synthesized and evaluated for their antimycobacterial activity.Conclusion:The synthesis is efficient and straightforward, involving only two successiveN-alkylations. The anti-TB assay reveal that our compounds have an excellent anti-TB activity against both replicating and nonreplicatingMtb, are not cytotoxic, exhibited a very good intracellular activity and are active against drug-resistantMtbstrains, 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. Aim: Results: bis Conclusion: N Mtb Mtb | ||
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