Effect of structure on antibiotic action of new 9-(ethylthio)acridines
Six new 9-(ethylthio)acridine derivatives were examined for antibacterial and antifungal activities with 10 bacterial and 8 yeast strains. The only active compounds were 2-and 3-amino derivatives. The observed MICs (mg/L) for 2-amino-9-(ethylthio)acridine (possessing the highest biological activity)...
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| Veröffentlicht in: | Folia microbiologica 2002-01, Vol.47 (2), p.118-120 |
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| container_title | Folia microbiologica |
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| creator | Nesměrák, K Pospíšek, M Zikánová, B Němec, I Barbe, J Gabriel, J |
| description | Six new 9-(ethylthio)acridine derivatives were examined for antibacterial and antifungal activities with 10 bacterial and 8 yeast strains. The only active compounds were 2-and 3-amino derivatives. The observed MICs (mg/L) for 2-amino-9-(ethylthio)acridine (possessing the highest biological activity) were 12 (P. mirabilis), 30 (B. subtillis), 60 (C. freundii), 90 (E. coli), 128 (E. vulneris) and 500 (S. marcescens andS. aureus). Both amino derivatives have also lowest half-wave potential (E ₁/₂) and field Swain-Lupton constants (describing oxidoreduction behavior) what supports the importance of acridine ion formation in the mechanism of antimicrobial action. |
| doi_str_mv | 10.1007/BF02817668 |
| format | Article |
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The only active compounds were 2-and 3-amino derivatives. The observed MICs (mg/L) for 2-amino-9-(ethylthio)acridine (possessing the highest biological activity) were 12 (P. mirabilis), 30 (B. subtillis), 60 (C. freundii), 90 (E. coli), 128 (E. vulneris) and 500 (S. marcescens andS. aureus). Both amino derivatives have also lowest half-wave potential (E ₁/₂) and field Swain-Lupton constants (describing oxidoreduction behavior) what supports the importance of acridine ion formation in the mechanism of antimicrobial action.</description><identifier>ISSN: 0015-5632</identifier><identifier>EISSN: 1874-9356</identifier><identifier>DOI: 10.1007/BF02817668</identifier><identifier>PMID: 12058388</identifier><identifier>CODEN: FOMIAZ</identifier><language>eng</language><publisher>Praha: Springer Netherlands</publisher><subject>Acridine ; acridines ; Acridines - chemical synthesis ; Acridines - chemistry ; Acridines - pharmacology ; Anti-Bacterial Agents ; Anti-Infective Agents - chemical synthesis ; Anti-Infective Agents - chemistry ; Anti-Infective Agents - pharmacology ; Antibacterial agents ; antibiotics ; Antibiotics. Antiinfectious agents. Antiparasitic agents ; antifungal properties ; Bacteria ; Bacteria - drug effects ; Biological activity ; Biological and medical sciences ; Derivatives ; E coli ; Escherichia coli ; Fungicides ; Medical sciences ; Microbial Sensitivity Tests ; Molecular Structure ; Pharmacology. Drug treatments ; Proteus mirabilis ; Staphylococcus aureus ; Structure-Activity Relationship ; Yeasts ; Yeasts - drug effects</subject><ispartof>Folia microbiologica, 2002-01, Vol.47 (2), p.118-120</ispartof><rights>2002 INIST-CNRS</rights><rights>Folia Microbiologica 2002.</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c396t-ade905bff0adeb91d859dc3d1c576c512e93d33311343ee553144e9cc443cfa33</citedby><cites>FETCH-LOGICAL-c396t-ade905bff0adeb91d859dc3d1c576c512e93d33311343ee553144e9cc443cfa33</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>314,780,784,27924,27925</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=14188939$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/12058388$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Nesměrák, K</creatorcontrib><creatorcontrib>Pospíšek, M</creatorcontrib><creatorcontrib>Zikánová, B</creatorcontrib><creatorcontrib>Němec, I</creatorcontrib><creatorcontrib>Barbe, J</creatorcontrib><creatorcontrib>Gabriel, J</creatorcontrib><title>Effect of structure on antibiotic action of new 9-(ethylthio)acridines</title><title>Folia microbiologica</title><addtitle>Folia Microbiol (Praha)</addtitle><description>Six new 9-(ethylthio)acridine derivatives were examined for antibacterial and antifungal activities with 10 bacterial and 8 yeast strains. The only active compounds were 2-and 3-amino derivatives. The observed MICs (mg/L) for 2-amino-9-(ethylthio)acridine (possessing the highest biological activity) were 12 (P. mirabilis), 30 (B. subtillis), 60 (C. freundii), 90 (E. coli), 128 (E. vulneris) and 500 (S. marcescens andS. aureus). Both amino derivatives have also lowest half-wave potential (E ₁/₂) and field Swain-Lupton constants (describing oxidoreduction behavior) what supports the importance of acridine ion formation in the mechanism of antimicrobial action.</description><subject>Acridine</subject><subject>acridines</subject><subject>Acridines - chemical synthesis</subject><subject>Acridines - chemistry</subject><subject>Acridines - pharmacology</subject><subject>Anti-Bacterial Agents</subject><subject>Anti-Infective Agents - chemical synthesis</subject><subject>Anti-Infective Agents - chemistry</subject><subject>Anti-Infective Agents - pharmacology</subject><subject>Antibacterial agents</subject><subject>antibiotics</subject><subject>Antibiotics. Antiinfectious agents. Antiparasitic agents</subject><subject>antifungal properties</subject><subject>Bacteria</subject><subject>Bacteria - drug effects</subject><subject>Biological activity</subject><subject>Biological and medical sciences</subject><subject>Derivatives</subject><subject>E coli</subject><subject>Escherichia coli</subject><subject>Fungicides</subject><subject>Medical sciences</subject><subject>Microbial Sensitivity Tests</subject><subject>Molecular Structure</subject><subject>Pharmacology. 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| ispartof | Folia microbiologica, 2002-01, Vol.47 (2), p.118-120 |
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| subjects | Acridine acridines Acridines - chemical synthesis Acridines - chemistry Acridines - pharmacology Anti-Bacterial Agents Anti-Infective Agents - chemical synthesis Anti-Infective Agents - chemistry Anti-Infective Agents - pharmacology Antibacterial agents antibiotics Antibiotics. Antiinfectious agents. Antiparasitic agents antifungal properties Bacteria Bacteria - drug effects Biological activity Biological and medical sciences Derivatives E coli Escherichia coli Fungicides Medical sciences Microbial Sensitivity Tests Molecular Structure Pharmacology. Drug treatments Proteus mirabilis Staphylococcus aureus Structure-Activity Relationship Yeasts Yeasts - drug effects |
| title | Effect of structure on antibiotic action of new 9-(ethylthio)acridines |
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