2361-62-8Relevant articles and documents
Novel berberine triazoles: Synthesis, antimicrobial evaluation and competitive interactions with metal ions to Human Serum Albumin
Zhang, Shao-Lin,Chang, Juan-Juan,Damu, Guri L.V.,Fang, Bo,Zhou, Xiang-Dong,Geng, Rong-Xia,Zhou, Cheng-He
, p. 1008 - 1012 (2013/03/14)
A series of novel berberine triazoles were synthesized and characterized by IR, NMR, MS and HRMS spectra. All target compounds and their precursors were screened for antimicrobial activities in vitro against four Gram-positive bacteria, four Gram-negative bacteria and two fungal strains. Bioactive assay indicated that most of the prepared compounds exhibited good antibacterial and antifungal activities with low MIC values ranging from 2 to 64 μg/mL, which were comparable to or even better than the reference drugs Berberine, Chloromycin, Norfloxacin and Fluconazole. The competitive interactions between compound 5a and metal ions to Human Serum Albumin (HSA) revealed that the participation of Mg2+ and Fe3+ ions in compound 5a-HSA association could result in the concentration increase of free compound 5a, shorten the storage time and half-life of compound 5a in the blood, thus improving its antimicrobial efficacy.
Berberine azoles as antimicrobial agents: Synthesis, biological evaluation and their interactions with human serum albumin
Zhang, Shao-Lin,Chang, Juan-Juan,Damu, Guri L. V.,Geng, Rong-Xia,Zhou, Cheng-He
, p. 839 - 846 (2013/08/26)
A series of berberine azoles was synthesized and characterized by NMR, IR, MS and HRMS spectroscopy. All the newly prepared compounds were screened for their antimicrobial activities. Bioactivity assays manifested that most of the berberine azoles exhibited good antimicrobial activities. Especially compound 7a displayed remarkable anti-Proteus vulgaris and anti-Candida mycoderma efficacies, which were comparable to or even better than for the reference drugs. The binding behavior of compound 7a to human serum albumin (HSA) revealed that hydrophobic interactions and hydrogen bonds play important roles in the association of compound 7a with HSA. Molecular docking experiments showed that compound 7a has moderate affinity to HSA, and the theoretical calculations were in accordance with the experimental results. The Royal Society of Chemistry 2013.