A series of spiro[acenaphthylene-1,2′-pyrrolidine] derivatives (4a-j) were synthesized by highly efficient one-pot three-component reaction of acenaphthenequinone, sarcosine and Knoevenagel adduct in 2,2,2-trifluoroethanol as a reusable green solvent. All the synthesized compounds were screened for their ‘in vitro’ antimalarial activity against the growth of Plasmodium falciparum, the malaria causing parasite. Some of them showed antimalarial activity with IC50 values as low as 0.003 and 0.005 mg mL-1 . The compounds were evaluated for their antibacterial activity against Escherichia coli, Staphylococcus aureus, Pseudomonas aeruginosa and Streptococcus pyogenes and for antifungal activity against Candida albicans, Aspergillus niger, and Aspergillus clavatus. Some of the compounds exhibited excellent antibacterial activity and compounds 4c and 4e demonstrated significant antifungal activities than the standard drugs.
Key words: Spiro[acenaphthylene-1,2’-pyrrolidines], Knoevenagel adduct, trifluoroethanol, antimalarial and antimicrobial activities.
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