Synthesis and biological activities of novel amine-derived bis-azoles as potential antibacterial and antifungal agents
Abstract
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 in vitro against six representative bacterial strains and two fungal strains. Bioactive results indicated that some synthesized compounds exhibited moderate or even better activities in comparison with the reference drugs. Especially, bis-imidazole 5b and its salts gave significant antibacterial efficacy against all tested bacteria strains including MRSA, while bis-triazoles 4b-c and their corresponding salts exhibited better activities against Candida albicans, Bacillus proteus than standard drugs Fluconazole and Norfloxacin respectively. Unexpectedly, bis-bromides 3a-f presented excellent activities against all tested microbial strains.
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Derived compounds of traditional antifungal structures include some with better antimicrobial action than the original structures.
“The second group involves derived compounds of traditional antifungal structures [54, 55] where some of them present better antimicrobial action than the original structures [55, 140].”
From <i>Candida</i>Infections, Causes, Targets, and Resistance Mechanisms: Traditional and Alternative Antifungal Agents (2013) · cites this paper as [55]
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- Authors
- Fang, B., Zhou, C.-H., & Rao, X.-C.
- Affiliations
- Southwest University (CN)
- Corresponding author
- Zhou, Cheng-He
- Venue
- European Journal of Medicinal Chemistry
- Publisher
- Elsevier BV
- Published
- 2010-09
- Volume
- 45
- Issue
- 9
- Pages
- 4388-4398
- ISSN
- 0223-5234 (ISSN-L)
- OpenAlex
- W2045044814
- Cited by
- 125
- References
- 32
- Citations by year
- 2026: 3 · 2025: 7 · 2024: 5 · 2023: 5 · 2022: 7 · 2021: 6 · 2020: 10 · 2019: 8 · 2018: 10 · 2017: 5 · 2016: 13 · 2015: 5 · 2014: 13 · 2013: 11 · 2012: 10
- FWCI
- 4.43
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- European Journal of Medicinal Chemistry (publishedVersion)
- PubMed (publishedVersion)
- Funders
- Southwest University
- Topics
- Physical Sciences › Chemistry › Organic Chemistry › Synthesis and Characterization of Heterocyclic Compounds
- Physical Sciences › Chemistry › Organic Chemistry › Structural and Chemical Analysis of Organic and Inorganic Compounds
- Physical Sciences › Chemistry › Organic Chemistry › Synthesis and Reactions of Organic Compounds
- Keywords
- amine derivatives, antibacterial agents, antifungal agents, bis-triazoles, methicillin-resistant Staphylococcus aureus, Candida albicans, Bacillus proteus, antimicrobial activity, structure-activity relationship
- MeSH terms
- Amines, Anti-Bacterial Agents, Antifungal Agents, Azoles, Bacteria, Fungi, Microbial Sensitivity Tests, Magnetic Resonance Spectroscopy, Structure-Activity Relationship
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