title: Synthesis and in vitro antiplasmodial activities of fluoroquinolone analogs.
abstract: Fluoroquinolone analogs were synthesized by simple alkylation followed by click chemistry and evaluated for their antimalarial in vitro against chloroquine sensitive strain of Plasmodium falciparum while ciprofloxacin was used as standard. Our results showed that the compound 12 was found most active with IC(50) value of 1.33 μg/mL while ciprofloxacin showed IC(50) = 8.81 μg/mL. Therefore, screening of either known or unknown quinolone/fluoroquinolone analogs are worthwhile to find more potent antimalarial drugs which might prove useful in the treatment of mild or severe malaria in human either alone or in combination with existing antimalarial drugs.
authors.affiliation: Chemical Biology Laboratory, Department of Chemistry, University of Delhi, Mall Road, Delhi 110007, India.
authors.forename: Sandeep K
authors.initials: SK
authors.lastname: Dixit
authors.forename: Nidhi
authors.initials: N
authors.lastname: Mishra
authors.forename: Manish
authors.initials: M
authors.lastname: Sharma
authors.forename: Shailja
authors.initials: S
authors.lastname: Singh
authors.forename: Alka
authors.initials: A
authors.lastname: Agarwal
authors.forename: Satish K
authors.initials: SK
authors.lastname: Awasthi
authors.forename: V K
authors.initials: VK
authors.lastname: Bhasin
mesh_terms: D000962:Antimalarials / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology* / Q000633:toxicity; D002470:Cell Survival / Q000187:drug effects; D060326:Chemistry Techniques, Synthetic; D024841:Fluoroquinolones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology* / Q000633:toxicity; D057809:HEK293 Cells; D006801:Humans; D020128:Inhibitory Concentration 50; D010963:Plasmodium falciparum / Q000187:drug effects*; D014230:Triazoles / Q000737:chemistry
chemical_list: D000962:Antimalarials; D024841:Fluoroquinolones; D014230:Triazoles