title: Synthesis and in vitro antitubercular activity of ferrocene-based hydrazones.
abstract: We report here the synthesis and in vitro antitubercular activity of a new series of ferrocenyl derivatives. The quinoline-ferrocene hybrid 5 exhibited significant activity (MIC=2.5-5 μg/ml) against Mycobacterium tuberculosis. Results indicate that such hybrid compounds provide an efficient approach for future pharmacological developments to fight against tuberculosis. Moreover, the antimalarial drug candidate ferroquine (FQ, SSR97193) was also evaluated mainly because of its structural similarity. FQ was found to display moderate inhibitory activity (MIC=10-15 μg/ml) against M. tuberculosis. This new drug may offer an interesting alternative in endemic area where malaria and tuberculosis coexist.
authors.affiliation: Department of Chemistry and Institute of Infectious Disease & Molecular Medicine, University of Cape Town, Rondebosch 7701, South Africa.
authors.forename: Aman
authors.initials: A
authors.lastname: Mahajan
authors.forename: Laurent
authors.initials: L
authors.lastname: Kremer
authors.forename: Stefan
authors.initials: S
authors.lastname: Louw
authors.forename: Yann
authors.initials: Y
authors.lastname: Guérardel
authors.forename: Yann
authors.initials: Y
authors.lastname: Guéradel
authors.forename: Kelly
authors.initials: K
authors.lastname: Chibale
authors.forename: Christophe
authors.initials: C
authors.lastname: Biot
mesh_terms: D000995:Antitubercular Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D005296:Ferrous Compounds / Q000737:chemistry*; D006835:Hydrazones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D000075163:Metallocenes; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D009169:Mycobacterium tuberculosis / Q000187:drug effects*
chemical_list: D000995:Antitubercular Agents; D005296:Ferrous Compounds; D006835:Hydrazones; D000075163:Metallocenes; C004998:ferrocene