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Microwave-assisted, rapid synthesis of 2-vinylquinolines and evaluation of their antimalarial activity.

ABSTRACT: A rapid and efficient synthesis of 2-vinylquinolines via trifluoromethanesulfonamidemediated olefination of 2-methylquinoline and aldehyde under microwave irradiation is reported. Biological evaluation of these scaffolds demonstrates that 2-vinylquinolines 3x - 3z possess excellent antimalarial activities against chloroquine-resistant Dd2 strain of Plasmodium falciparum (IC50 < 100 nM).

SUBMITTER: Huang G

PROVIDER: S-EPMC6892474 | biostudies-literature | 2019 Jun

REPOSITORIES: biostudies-literature

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Microwave-assisted, rapid synthesis of 2-vinylquinolines and evaluation of their antimalarial activity.

Huang Guang G Solano Claribel Murillo CM Su Yuxin Y Ezzat Nameer N Matsui Shino S Huang Liuyu L Chakrabarti Debopam D Yuan Yu Y

Tetrahedron letters 20190528 26

A rapid and efficient synthesis of 2-vinylquinolines via trifluoromethanesulfonamidemediated olefination of 2-methylquinoline and aldehyde under microwave irradiation is reported. Biological evaluation of these scaffolds demonstrates that 2-vinylquinolines 3x - 3z possess excellent antimalarial activities against chloroquine-resistant Dd2 strain of Plasmodium falciparum (IC50 < 100 nM). ...[more]

PMID: 31802783

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