title: 1H-1,2,3-triazole tethered mono- and bis-ferrocenylchalcone-β-lactam conjugates: synthesis and antimalarial evaluation.
abstract: A series of ferrocenylchalcone-β-lactam conjugates were synthesized and evaluated against 3D7 (CQ-Sensitive) and W2 (CQ-Resistant) strains of Plasmodium falciparum. The SAR studies revealed the dependence of activities at N-1 substituent of β-lactam ring with compounds being more potent on resistant strain. The compound 9f and 9l with N-cyclohexyl substituent proved to be the most potent and non-cytotoxic among the series exhibiting IC50 values of 2.36 and 2.43 μM respectively, against W2 strain of P. falciparum.
authors.affiliation: Department of Chemistry, Guru Nanak Dev University, Amritsar 143005, India.
authors.forename: Kewal
authors.initials: K
authors.lastname: Kumar
authors.affiliation: Unité de Parasitologie et d'Entomologie, Département de Microbiologie, Institut de Recherche Biomédicale des Armées, Brétigny sur Orge, France; Aix Marseille Université, Unité de Recherche sur les Maladies Infectieuses et Tropicales Emergentes, UM 63, CNRS 7278, IRD 198, Inserm 1095, Marseille, France; Centre National de Référence du Paludisme, Marseille, France.
authors.forename: Bruno
authors.initials: B
authors.lastname: Pradines
authors.affiliation: Aix Marseille Université, Unité de Recherche sur les Maladies Infectieuses et Tropicales Emergentes, UM 63, CNRS 7278, IRD 198, Inserm 1095, Marseille, France; Centre National de Référence du Paludisme, Marseille, France; Equipe Résidente de Recherche en Infectiologie Tropicale, Institut de Recherche Biomédicale des Armées, Hôpital d'Instruction des Armées Laveran, Marseille, France.
authors.forename: Marilyn
authors.initials: M
authors.lastname: Madamet
authors.affiliation: Aix Marseille Université, Unité de Recherche sur les Maladies Infectieuses et Tropicales Emergentes, UM 63, CNRS 7278, IRD 198, Inserm 1095, Marseille, France; Centre National de Référence du Paludisme, Marseille, France; Equipe Résidente de Recherche en Infectiologie Tropicale, Institut de Recherche Biomédicale des Armées, Hôpital d'Instruction des Armées Laveran, Marseille, France.
authors.forename: Rémy
authors.initials: R
authors.lastname: Amalvict
authors.affiliation: Department of Chemistry, Guru Nanak Dev University, Amritsar 143005, India. Electronic address: vipan_org@yahoo.com.
authors.forename: Vipan
authors.initials: V
authors.lastname: Kumar
mesh_terms: D000962:Antimalarials / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D006367:HeLa Cells; D006801:Humans; D015394:Molecular Structure; D021261:Parasitic Sensitivity Tests; D010963:Plasmodium falciparum / Q000187:drug effects*; D013329:Structure-Activity Relationship; D014230:Triazoles / Q000737:chemistry / Q000494:pharmacology*; D047090:beta-Lactams / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D000962:Antimalarials; D014230:Triazoles; D047090:beta-Lactams
keywords: 1H-1,2,3-triazoles; Click chemistry; Ferrcenylchalcone-β-lactam conjugates; Plasmodium falciparum; Structure–activity relationship