title: Synthesis and bioactive evaluation of novel hybrids of metronidazole and berberine as new type of antimicrobial agents and their transportation behavior by human serum albumin.
abstract: A series of novel hybrids of metronidazole and berberine as new type of antimicrobial agents were synthesized and characterized by (1)H NMR, (13)C NMR, IR, MS and HRMS spectra. Bioactive assay manifested that most of the prepared compounds exhibited effective antibacterial and antifungal activities and some showed comparable or superior potency against Methicillin-resistant Staphylococcus aureus to reference drugs Norfloxacin, Chloromycin and Berberine. The transportation behavior of human serum albumin (HSA) to the highly active compound 5g was evaluated and revealed that the association of imidazole derivative 5g with HSA was spontaneous and the electrostatic interactions played important roles in the transportation of HSA to 5g. The calculated parameters indicated that compound 5g could be effectively stored and carried by HSA.
authors.affiliation: Laboratory of Bioorganic & Medicinal Chemistry, School of Chemistry and Chemical Engineering, Southwest University, Chongqing 400715, PR China.
authors.forename: Ling
authors.initials: L
authors.lastname: Zhang
authors.forename: Juan-Juan
authors.initials: JJ
authors.lastname: Chang
authors.forename: Shao-Lin
authors.initials: SL
authors.lastname: Zhang
authors.forename: Guri L V
authors.initials: GL
authors.lastname: Damu
authors.forename: Rong-Xia
authors.initials: RX
authors.lastname: Geng
authors.forename: Cheng-He
authors.initials: CH
authors.lastname: Zhou
mesh_terms: D000890:Anti-Infective Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D001419:Bacteria / Q000187:drug effects*; D001599:Berberine / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D001665:Binding Sites; D001692:Biological Transport; D005658:Fungi / Q000187:drug effects*; D006801:Humans; D009682:Magnetic Resonance Spectroscopy; D008795:Metronidazole / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D015394:Molecular Structure; D012709:Serum Albumin / Q000493:pharmacokinetics; D013816:Thermodynamics
chemical_list: D000890:Anti-Infective Agents; D012709:Serum Albumin; D001599:Berberine; D008795:Metronidazole