title: Urea/oxalamide tethered β-lactam-7-chloroquinoline conjugates: synthesis and in vitro antimalarial evaluation.
abstract: The manuscript pertains to the synthesis of urea/oxalamide tethered β-lactam-7-chloroquinoline conjugates with well modulated chain lengths and their antimalarial evaluation. The results reveal the dependence of activity profiles on the N-1 substituent of the β-lactam ring, the nature of the linker as well as the length of the alkyl chain. The most potent of the tested compounds showed an IC50 of 34.97 nM against chloroquine resistant W2 strain of Plasmodium falciparum.
authors.affiliation: Department of Chemistry, Guru Nanak Dev University, Amritsar 143005, Punjab, India.
authors.forename: Pardeep
authors.initials: P
authors.lastname: Singh
authors.affiliation: Department of Chemistry, Guru Nanak Dev University, Amritsar 143005, Punjab, India.
authors.forename: Raghu
authors.initials: R
authors.lastname: Raj
authors.affiliation: Department of Chemistry, Durban University of Technology, Durban 4000, South Africa.
authors.forename: Parvesh
authors.initials: P
authors.lastname: Singh
authors.affiliation: Department of Medicine, University of California, San Francisco, CA, USA.
authors.forename: Jiri
authors.initials: J
authors.lastname: Gut
authors.affiliation: Department of Medicine, University of California, San Francisco, CA, USA.
authors.forename: Philip J
authors.initials: PJ
authors.lastname: Rosenthal
authors.affiliation: Department of Chemistry, Guru Nanak Dev University, Amritsar 143005, Punjab, India. Electronic address: vipan_org@yahoo.com.
authors.forename: Vipan
authors.initials: V
authors.lastname: Kumar
mesh_terms: D000962:Antimalarials / Q000737:chemistry / Q000494:pharmacology*; D002738:Chloroquine / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D016778:Malaria, Falciparum / Q000188:drug therapy; D010072:Oxamic Acid / Q000031:analogs & derivatives / Q000494:pharmacology; D010963:Plasmodium falciparum / Q000187:drug effects*; D013329:Structure-Activity Relationship; D014508:Urea / Q000031:analogs & derivatives / Q000494:pharmacology*; D047090:beta-Lactams / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D000962:Antimalarials; D047090:beta-Lactams; D002738:Chloroquine; D014508:Urea; D010072:Oxamic Acid
keywords: Antimalarial evaluation; Structure–activity relationship; Urea/oxalamide linker; β-Lactam-7-chloroquinoline conjugates