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Original Article

ECB. 2013; 2(12): 1004-1008


AN EFFICIENT SYNTHESIS AND BIOLOGICAL EVALUATION OF SPIRO[ACENAPHTHYLENE-1,2′-PYRROLIDINE] DERIVATIVES AS POTENT ANTI-INFECTIVE AGENTS

Anshu Dandia, Sukhbeer Kumari, Pragya Soni.




Abstract

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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