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Substituted 1,3-dioxoisoindoline-4-aminoquinolines coupled via amide linkers: Synthesis, antiplasmodial and cytotoxic evaluation.

Abstract：

:Synthesis of C-5-substituted 1,3-dioxoisoindoline-4-aminoquinolines having amide group as a spacer was developed with an intent to evaluate their antiplasmodial activities. The synthesized dioxoisoindoline-aminoquinolines tethered with β-alanine as a spacer and secondary amine as substituent displayed good anti-plasmodial activities. Compound 7j, with an optimum combination of β-alanine and an ethyl chain length as linker along with diethylamine as the secondary amine counterpart at dioxoisoindoline proved to be most potent and non-cytotoxic with IC50 of 0.097 µM against W2 strain of P. falciparum and a selective index of >2000.

journal_name

Bioorg Chem

journal_title

Bioorganic chemistry

authors

Rani A,Legac J,Rosenthal PJ,Kumar V

doi

10.1016/j.bioorg.2019.04.006

subject

Has Abstract

pub_date

2019-07-01 00:00:00

pages

102912

eissn

0045-2068

issn

1090-2120

pii

S0045-2068(19)30195-6

journal_volume

88

pub_type

杂志文章

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