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

• Synthesis of β-amino alcohol tethered isatin 4-aminoquinoline conjugates.
• Antimalarial evaluation against W2 strains of Plasmodium falciparum.
• Most active and non-cytotoxic conjugate exhibited an IC50 11.7 nM.

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.

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