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A novel synthesis of 2-arylbenzimidazoles in molecular sieves-MeOH system and their antitubercular activity
AK. Chaturvedi, AK. Verma, JP. Thakur, S. Roy, S. Bhushan Tripathi, BS. Kumar, S. Khwaja, NK. Sachan, A. Sharma, D. Chanda, K. Shanker, D. Saikia, AS. Negi,
Bioorganic & medicinal chemistry.
2018 ;
26 (15) :
4551-4559.
[pub] 20180801
Jazyk angličtina Země Anglie, Velká Británie
Typ dokumentu časopisecké články, práce podpořená grantem
Perzistentní odkaz
https://www.medvik.cz/link/bmc19012474
- MeSH
- antituberkulotika chemická syntéza farmakologie MeSH
- aplikace orální MeSH
- bakteriální proteiny antagonisté a inhibitory metabolismus MeSH
- DNA gyráza chemie metabolismus MeSH
- imidazoly chemie farmakologie MeSH
- mikrobiální testy citlivosti MeSH
- Mycobacterium tuberculosis účinky léků MeSH
- myši MeSH
- simulace molekulového dockingu MeSH
- tělesná hmotnost účinky léků MeSH
- terciární struktura proteinů MeSH
- vazebná místa MeSH
- vztahy mezi strukturou a aktivitou MeSH
- zvířata MeSH
- Check Tag
- myši MeSH
- zvířata MeSH
- Publikační typ
- časopisecké články MeSH
- práce podpořená grantem MeSH
Arylbenzimidazoles have been synthesized as antimycobacterial agents. An efficient synthesis has been developed for 2-arylbenzimidazoles from o-phenylenediamines and aromatic aldehydes in molecular sieves-methanol system. The methodology is straightforward to get 2-arylbenzimidazoles (3a-3z) in excellent yields with high chemoselectivity over 2-aryl-1-benzylbenzimidazoles (4a-4z). All these benzimidazole analogues were evaluated against M. tuberculosis in BACTEC radiometric assay. The compounds 4y and 4z exhibited potential antitubercular activity against M. tuberculosis H37RV, MIC at 16 µM and 24 µM respectively. The best compound of the series i.e. compound 4y was well tolerated by Swiss-albino mice in acute oral toxicity. Compound 4y possessing a diarylbenzimidazole core, can further be optimized for better activity.
Citace poskytuje Crossref.org
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