title: The synthesis and activities of novel mononuclear or dinuclear cyclen complexes bearing azole pendants as antibacterial and antifungal agents.
abstract: A series of novel compounds containing 1,4,7,10-tetraazacyclododecane and azoles were synthesized and characterized by (1)H NMR, MS and elemental analysis. Bioactive assay manifested that some target compounds, such as 11a, 11b and 11d, displayed good and broad spectrum antimicrobial activities with relative low MIC values against most of tested strains. These dinuclear complexes gave comparable or even better antimicrobial efficiencies than the reference drugs Fluconazole and Chloromycin. The result showed that the metal ions were the key factors to enhance the antimicrobial activities for mononuclear or dinuclear complexed in varying degrees. The interaction evaluation of compound 11b with bovine serum albumin (BSA) as an example was tested by fluorescence method. The thermodynamic parameters indicated that the hydrogen bonds and van der waals forces played the major roles in the strong association between dinuclear compound and BSA. The CCK-8 tests also confirmed the safeties of these dinuclear compounds in vitro.
authors: School of Chemical Engineering, Chongqing University of Technology, Chongqing 400054, People's Republic of China. Electronic address: lishuo@cqut.edu.cn.
authors: Shuo
authors: S
authors: Li
authors: Department of Chemistry, Leshan Normal University, Leshan, Sichuan 614000, People's Republic of China.
authors: Jia-Xuan
authors: JX
authors: Chen
authors: Department of Chemistry, Leshan Normal University, Leshan, Sichuan 614000, People's Republic of China. Electronic address: qxxiang711@163.com.
authors: Qing-Xiang
authors: QX
authors: Xiang
authors: Department of Chemistry, Leshan Normal University, Leshan, Sichuan 614000, People's Republic of China.
authors: Li-Qun
authors: LQ
authors: Zhang
authors: Laboratory of Bioorganic & Medicinal Chemistry, School of Chemistry and Chemical Engineering, Southwest University, Chongqing 400715, People's Republic of China.
authors: Cheng-He
authors: CH
authors: Zhou
authors: School of Chemical Engineering, Chongqing University of Technology, Chongqing 400054, People's Republic of China.
authors: Jia-Qing
authors: JQ
authors: Xie
authors: School of Chemical Engineering, Chongqing University of Technology, Chongqing 400054, People's Republic of China.
authors: Lan
authors: L
authors: Yu
authors: School of Chemical Engineering, Chongqing University of Technology, Chongqing 400054, People's Republic of China.
authors: Fang-Zhen
authors: FZ
authors: Li
mesh_terms: D000818:Animals; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D000935:Antifungal Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D001393:Azoles / Q000737:chemistry*; D002417:Cattle; D000080027:Cyclams; D004305:Dose-Response Relationship, Drug; D005658:Fungi / Q000187:drug effects; D006090:Gram-Negative Bacteria / Q000187:drug effects; D006094:Gram-Positive Bacteria / Q000187:drug effects; D006571:Heterocyclic Compounds / Q000737:chemistry* / Q000494:pharmacology*; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D012710:Serum Albumin, Bovine / Q000737:chemistry; D013329:Structure-Activity Relationship
chemical_list: D000900:Anti-Bacterial Agents; D000935:Antifungal Agents; D001393:Azoles; D000080027:Cyclams; D006571:Heterocyclic Compounds; D012710:Serum Albumin, Bovine; C038072:cyclen
keywords: Antibacterial; Antifungal; Azoles; Cyclen; Fluorescence spectrum