4233-26-5Relevant 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.
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
Zhang, Ling,Chang, Juan-Juan,Zhang, Shao-Lin,Damu, Guri L.V.,Geng, Rong-Xia,Zhou, Cheng-He
, p. 4158 - 4169 (2013/07/27)
A series of novel hybrids of metronidazole and berberine as new type of antimicrobial agents were synthesized and characterized by 1H NMR, 13C 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.
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.
Synthesis and biological activities of novel amine-derived bis-azoles as potential antibacterial and antifungal agents
Fang, Bo,Zhou, Cheng-He,Rao, Xian-Cai
experimental part, p. 4388 - 4398 (2010/10/02)
A series of novel amine-derived bis-azole compounds were designed by the systematical structural modification of Fluconazole and synthesized by a convenient and efficient method, and the antimicrobial activities for all prepared compounds were evaluated i
ALKYNYL CONTAINING HYDROXAMIC ACID DERIVATIVES, THEIR PREPARATION AND THEIR USE AS MATRIX METALLOPROTEINASE (MMP) INHIBITORS / TNF-ALPHA CONVERTING ENZYME (TACE) INHIBITORS
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Page/Page column 28, (2010/02/14)
Compounds of the formula:useful in the treatment of arthritis, tumor metastasis, tissue ulceration, abnormal wound healing, periodontal disease, bone disease, diabetes (insulin resistance) and HIV infection.