title: Synthesis and in vitro anti-tubercular evaluation of 1,2,3-triazole tethered β-lactam-ferrocene and β-lactam-ferrocenylchalcone chimeric scaffolds.
abstract: Twenty different triazoles were prepared to probe the anti-tubercular structure-activity relationships (SAR) within the β-lactam-ferrocene-triazole conjugate family. The compounds have been synthesized by copper-catalyzed "click chemistry". In vitro anti-tubercular activity was determined for each compound but the synthesized hybrids failed to inhibit Mycobacterium tuberculosis growth even at high doses. The manuscript assumes significance as this is the first report on the inclusion of ferrocene nucleus in the well established β-lactam family via triazole linkers with reputed physicochemical profiles.
authors.affiliation: Department of Chemistry, Guru Nanak Dev University, Amritsar-143005, Punjab, India.
authors.forename: Kewal
authors.initials: K
authors.lastname: Kumar
authors.forename: Pardeep
authors.initials: P
authors.lastname: Singh
authors.forename: Laurent
authors.initials: L
authors.lastname: Kremer
authors.forename: Yann
authors.initials: Y
authors.lastname: Guérardel
authors.forename: Christophe
authors.initials: C
authors.lastname: Biot
authors.forename: Vipan
authors.initials: V
authors.lastname: Kumar
mesh_terms: D000995:Antitubercular Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D002599:Chalcone / Q000031:analogs & derivatives* / Q000737:chemistry*; D060326:Chemistry Techniques, Synthetic; D005296:Ferrous Compounds / Q000737:chemistry*; D000075163:Metallocenes; D008826:Microbial Sensitivity Tests; D009169:Mycobacterium tuberculosis / Q000187:drug effects; D014230:Triazoles / Q000737:chemistry*; D047090:beta-Lactams / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*
chemical_list: D000995:Antitubercular Agents; D005296:Ferrous Compounds; D000075163:Metallocenes; D014230:Triazoles; D047090:beta-Lactams; D002599:Chalcone; C004998:ferrocene