| Imidazo- and triazoloquinolones as antibacterial agents. Synthesis and structure-activity relationships. | |
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MedLine Citation:
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PMID: 8582014 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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4,5-Disubstituted 6-cyclopropyl-6,9-dihydro-9-oxo-1H-imidazo (30-32) and triazolo[4,5-f]quinoline-8-carboxylic acids (33-35) were synthesized starting from 5,6-diaminoquinolones 25. The imidazoquinolones 30-32 were equal or superior to the corresponding triazoloquinolone analogues 33-35 in in vitro antibacterial activity. As for the C-5 substituents, a fluorine atom was the most favorable of the three groups, H, F, and Cl. Among the compounds prepared, 4-(cyclic amino)-5-fluoro-imidazoquinolones 31 a-d showed potent and well-balanced antibacterial activity against both gram-positive and gram-negative bacteria. Structure-activity relationships for the C-4 substituents (cyclic amino groups) were also examined in detail. |
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Authors:
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M Fujita; H Egawa; M Kataoka; T Miyamoto; J Nakano; J Matsumoto |
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Publication Detail:
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Type: Journal Article |
Journal Detail:
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Title: Chemical & pharmaceutical bulletin Volume: 43 ISSN: 0009-2363 ISO Abbreviation: Chem. Pharm. Bull. Publication Date: 1995 Dec |
Date Detail:
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Created Date: 1996-03-21 Completed Date: 1996-03-21 Revised Date: 2003-11-14 |
Medline Journal Info:
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Nlm Unique ID: 0377775 Medline TA: Chem Pharm Bull (Tokyo) Country: JAPAN |
Other Details:
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Languages: eng Pagination: 2123-32 Citation Subset: IM |
Affiliation:
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Exploratory Research Laboratories, Dainippon Pharmaceutical Company, Osaka, Japan. |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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Animals Anti-Infective Agents / chemical synthesis*, pharmacology Bacteria / drug effects* Gram-Negative Bacteria / drug effects Gram-Positive Bacteria / drug effects Imidazoles / chemical synthesis*, pharmacology Male Mice Mice, Inbred Strains Microbial Sensitivity Tests Pseudomonas Infections / drug therapy Quinolones / chemical synthesis*, pharmacology Structure-Activity Relationship Triazoles / chemical synthesis*, pharmacology |
| Chemical | |
Reg. No./Substance:
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0/Anti-Infective Agents; 0/Imidazoles; 0/Quinolones; 0/Triazoles |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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