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- Title
Amalgamating Isatin/Indole/Nitroimidazole with 7‐chloroquinolines via azide‐alkyne cycloaddition: Synthesis, anti‐plasmodial, and cytotoxic evaluation.
- Authors
Kumar, Sumit; Saini, Anu; Legac, Jenny; Rosenthal, Philip J.; Raj, Raghu; Kumar, Vipan
- Abstract
The present paper describes the synthesis, anti‐plasmodial, and cytotoxic evaluation of 7‐chloroquinoline‐based conjugates with isatins/indoles/ nitroimidazoles, obtained via Cu‐promoted 1,3‐dipolar cycloadditions. On contemplating SAR of the synthesized series, the inclusion of indole and nitroimidazole‐core improved the anti‐plasmodial activities while the isatin seemed to have a lesser effect. The conjugate with a nitroimidazole‐core and hexyl chain length as a spacer between the two pharmacophores was found to be most potent among the synthesized series and displayed an IC50 of 0.12 µM and a selectivity index of 1748.
- Subjects
ISATIN; RING formation (Chemistry); ISOXAZOLIDINES; INDOLE; NITROIMIDAZOLES
- Publication
Chemical Biology & Drug Design, 2020, Vol 96, Issue 6, p1355
- ISSN
1747-0277
- Publication type
Article
- DOI
10.1111/cbdd.13738