Cited by 127Synthesis and Characterization of Heterocyclic CompoundsStructural and Chemical Analysis of Organic and Inorganic CompoundsSynthesis and Reactions of Organic Compounds

Synthesis and biological activities of novel amine-derived bis-azoles as potential antibacterial and antifungal agents

Fang, Bo, Zhou, Cheng-He, Rao, Xian-Cai·2010·European Journal of Medicinal Chemistry

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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Crossref · 10.1016/j.ejmech.2010.06.012

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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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