Issue 1, 2015

Synthesis of tetrazole compounds as a novel type of potential antimicrobial agents and their synergistic effects with clinical drugs and interactions with calf thymus DNA

Abstract

A series of tetrazole derivatives were synthesized and characterized by NMR, IR, MS and HRMS spectroscopy. The bioactive assay manifested that most of the target compounds exhibited good antifungal activity, especially compound 6g displayed comparable or even stronger antifungal efficiency in comparison with the reference drug Fluconazole. The combination of tetrazole derivative 6g with antibacterials Chloromycin and Norfloxacin, or antifungal Fluconazole respectively was more sensitive to methicillin-resistant MRSA and Fluconazole-insensitive Aspergillus flavus. Further research revealed that compound 6g could effectively intercalate into Calf Thymus DNA to form a 6g–DNA complex which might block DNA replication to exert its good antimicrobial activities.

Graphical abstract: Synthesis of tetrazole compounds as a novel type of potential antimicrobial agents and their synergistic effects with clinical drugs and interactions with calf thymus DNA

Supplementary files

Article information

Article type
Concise Article
Submitted
21 Jun 2014
Accepted
22 Sep 2014
First published
22 Sep 2014

Med. Chem. Commun., 2015,6, 147-154

Synthesis of tetrazole compounds as a novel type of potential antimicrobial agents and their synergistic effects with clinical drugs and interactions with calf thymus DNA

L. Dai, H. Zhang, S. Nagarajan, S. Rasheed and C. Zhou, Med. Chem. Commun., 2015, 6, 147 DOI: 10.1039/C4MD00266K

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