title: Antiplasmodial and cytotoxicity evaluation of 3-functionalized 2-azetidinone derivatives.
abstract: 3-Azido-, 3-amino- and 3-(1,2,3-triazol-1-yl)-β-lactams were synthesized and evaluated for their antiplasmodial activity against four strains of Plasmodium falciparum and KB cells for their cytotoxicity profiles. The presence of a cyclohexyl substituent at N-1 and a phenyl group on the triazole ring markedly improved the activity profiles of triazole-tethered β-lactam exhibiting IC(50) values of 1.13, 1.21 and 1.00 μM against 3D7, K1 and W2 strains respectively.
authors.affiliation: Department of Chemistry, Guru Nanak Dev University, Amritsar, India.
authors.forename: Pardeep
authors.initials: P
authors.lastname: Singh
authors.forename: Shaveta
authors.initials: S
authors.lastname: Sachdeva
authors.forename: Raghu
authors.initials: R
authors.lastname: Raj
authors.forename: Vipan
authors.initials: V
authors.lastname: Kumar
authors.forename: Mohinder P
authors.initials: MP
authors.lastname: Mahajan
authors.forename: Shereen
authors.initials: S
authors.lastname: Nasser
authors.forename: Livia
authors.initials: L
authors.lastname: Vivas
authors.forename: Jiri
authors.initials: J
authors.lastname: Gut
authors.forename: Phillip J
authors.initials: PJ
authors.lastname: Rosenthal
authors.forename: Tzu-Shean
authors.initials: TS
authors.lastname: Feng
authors.forename: Kelly
authors.initials: K
authors.lastname: Chibale
mesh_terms: D000962:Antimalarials / Q000138:chemical synthesis / Q000737:chemistry* / Q000633:toxicity; D001384:Azetidines / Q000138:chemical synthesis / Q000737:chemistry* / Q000633:toxicity; D045744:Cell Line, Tumor; D006801:Humans; D010963:Plasmodium falciparum / Q000187:drug effects; D014230:Triazoles / Q000737:chemistry; D047090:beta-Lactams / Q000737:chemistry
chemical_list: C116379:2-azetidinone; D000962:Antimalarials; D001384:Azetidines; D014230:Triazoles; D047090:beta-Lactams