Design, synthesis and in vitro anti-mycobacterial activities of homonuclear and heteronuclear bis-isatin derivatives
Xu Y, Guan J, Xu Z, Zhao S
Fitoterapia · 2018-04
Abstract
A series of novel homonuclear and heteronuclear bis-isatin derivatives tethered through ethylene were designed, synthesized and evaluated for their in vitro anti-mycobacterial activities against MTB H37Rv and MDR-TB. All hybrids exhibited potential anti-mycobacterial activities against MTB H37Rv and MDR-TB with MIC ranging from 16 to 256 μg/mL. In particular, the heteronuclear bis-isatin 4i (MIC: 25 and 16 μg/mL) was most active against MTB H37Rv and MDR-TB strains, and could act as a lead for further optimization.
MeSH terms
- Mycobacterium tuberculosis
- Ethylenes
- Isatin
- Antitubercular Agents
- Microbial Sensitivity Tests
- Molecular Structure
- Structure-Activity Relationship
- Drug Design