title: Search for new pharmacophore as antimalarial agent: synthesis and antimalarial activity of some 2(3H)-furanones bearing quinoline moiety.
abstract: A series of substituted 3-[(substituted-2-chloroquinolin-3-yl)methylene]-5-(substituted-phenyl)-furan-2(3H)-ones (4a-p) have been synthesized and evaluated for their in vitro antimalarial activity against P. falciparum. The title compounds were synthesized by condensing 3-(substituted-benzoyl)propionic acids (3a-d) with substituted 2-chloroquinoline-3-carbaldehydes (2a-d) following modified Perkin's reaction. Compounds 3-[2-chloro-6-methylquinolin-3-yl)methylene]-5-(2,4-dimethyl-phenyl)-furan-2(3H)-one (4n) and 3-[2-chloro-6-methoxyquinolin-3-yl)methylene]-5-(2,4-dimethyl-phenyl)-furan-2(3H)-one (4p) showed promising antimalarial activity with MIC of 10 microg/mL.
authors.affiliation: Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Jamia Hamdard, New Delhi-110062, India. drmmalam@gmail.com
authors.forename: Mohammad Mumtaz
authors.initials: MM
authors.lastname: Alam
authors.forename: Deba Priya
authors.initials: DP
authors.lastname: Sarkar
authors.forename: Ozair
authors.initials: O
authors.lastname: Alam
authors.forename: Asif
authors.initials: A
authors.lastname: Husain
authors.forename: Akranth
authors.initials: A
authors.lastname: Marella
authors.forename: Mymoona
authors.initials: M
authors.lastname: Akhtar
authors.forename: Mohammad
authors.initials: M
authors.lastname: Shaquiquzzaman
authors.forename: Suruchi
authors.initials: S
authors.lastname: Khanna
mesh_terms: D000962:Antimalarials / Q000138:chemical synthesis* / Q000494:pharmacology*; D005663:Furans / Q000138:chemical synthesis* / Q000494:pharmacology*; D009682:Magnetic Resonance Spectroscopy; D013058:Mass Spectrometry; D015394:Molecular Structure; D021261:Parasitic Sensitivity Tests; D010963:Plasmodium falciparum / Q000187:drug effects / Q000254:growth & development; D011804:Quinolines / Q000138:chemical synthesis* / Q000494:pharmacology*; D013055:Spectrophotometry, Infrared; D013329:Structure-Activity Relationship
chemical_list: D000962:Antimalarials; D005663:Furans; D011804:Quinolines