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A click chemistry approach for the synthesis of mono and bis aryloxy linked coumarinyl triazoles as anti-tubercular agents.
- Source :
-
European Journal of Medicinal Chemistry . Nov2015, Vol. 105, p194-207. 14p. - Publication Year :
- 2015
-
Abstract
- A series of mono and bis -triazole coumarin hybrids 6a–u and 9a–f respectively have been synthesized using 4-(azidomethyl)-2 H -chromen-2-ones 5a–i and aryl propargyl ethers 2a–c/8 employing Click chemistry modified protocol for Azide-Alkyne cycloadditions(CuAAC). Anti-tubercular screening showed moderate activity for mono aryloxy compounds 6a–u with MIC 50–100 μg/mL, whereas the bis compounds 9a–f were more effective with MICs between 0.2 and 12.5 μg/mL. Molecular modeling and 3D-QSAR measurements using CoMFA and Topomer CoMFA further supported the observed results. The bis compound 9b showed excellent activity with MIC value as low as 0.2 μg/mL. [ABSTRACT FROM AUTHOR]
Details
- Language :
- English
- ISSN :
- 02235234
- Volume :
- 105
- Database :
- Academic Search Index
- Journal :
- European Journal of Medicinal Chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 110632413
- Full Text :
- https://doi.org/10.1016/j.ejmech.2015.10.019