Microwave-promoted facile access to 4-aminoquinoline-phthalimides: Synthesis and anti-plasmodial evaluation

作者：Rani Anu; Singh Amandeep; Gut Jiri; Rosenthal Philip J; Kumar Vipan^*

来源：European Journal of Medicinal Chemistry, 2018, 143: 150-156.

DOI：10.1016/j.ejmech.2017.11.033

• 4-aminoquinoline-phthalimides
• Microwave synthesis
• Anti-plasmodial evaluation
• Cytotoxicity
• Selectivity index

Microwave promoted high yielding synthesis of 4-aminoquinoline-phthalimides was developed with an aim to evaluate their anti-plasmodial potential. The scaffolds with longer spacer length (n = 6, 8) between two pharmacophores and a halogen substituent on the phthalimide ring displayed good anti-plasmodial activity. Compound 5w, with an optimum combination of hexyl chain as spacer along with a tetra-bromophthalimide ring proved to be most potent and non-cytotoxic among the series exhibiting an IC50 value of 0.10 mu M.

• 出版日期2018-1-1