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?-amino-alcohol tethered 4-aminoquinoline-isatin conjugates: synthesis and antimalarial evaluation.

ABSTRACT: A series of ?-amino alcohol tethered 4-aminoquinoline-isatin conjugates were synthesized with the aim of probing their antimalarial structure activity relationship. Two of the most active conjugates (11b and 11f) exhibited antimalarial efficacy comparable to that of chloroquine, with IC50 values of 11.8 and 13.5 nM, respectively against chloroquine resistant W2 strain of Plasmodium falciparum and are devoid of any cytotoxicity.

SUBMITTER: Nisha 

PROVIDER: S-EPMC7115587 | biostudies-literature | 2014 Sep

REPOSITORIES: biostudies-literature

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β-amino-alcohol tethered 4-aminoquinoline-isatin conjugates: synthesis and antimalarial evaluation.

Nisha   Gut Jiri J   Rosenthal Philip J PJ   Kumar Vipan V  

European journal of medicinal chemistry 20140721

A series of β-amino alcohol tethered 4-aminoquinoline-isatin conjugates were synthesized with the aim of probing their antimalarial structure activity relationship. Two of the most active conjugates (11b and 11f) exhibited antimalarial efficacy comparable to that of chloroquine, with IC50 values of 11.8 and 13.5 nM, respectively against chloroquine resistant W2 strain of Plasmodium falciparum and are devoid of any cytotoxicity. ...[more]

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