| Antibacterial activity of 15-azasteroids alone and in combination with antibiotics. | |
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MedLine Citation:
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PMID: 179169 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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A new class of 15-azasteroid analogues has been synthesized and tested for antimicrobial activity. The compounds 1, 10, 11, 11a-tetrahydro-7-methoxy-11a-methyl-2H-naphth (1,2-g) indol (methoxyimine) and 1,10,11,11a-tetrahydro-11a-methyl-2H-naphth (1,2-g) indol-7-ol (hydroxyimine) inhibit the growth of Bacillus subtillis and Escherichia coli at concentrations as low as 10-5 M. Addition of either compound to the growth medium casued a rapid inhibition in the transport of radioactive glucose, uracil and several amino acids. The inhibition of growth and substrate transport was reversed following removl of the steroid from the medium. The evidence is consistent with a site of steroid action at the cell periphery. Combining the methoxyimine with polyor circulin at subinhibitory concentrations produced greatly enhanced antimicrobial activity against Pseudomonas fluorescens. Similar action was observed against B. subtilis when the azasteroid was combined with vancomycin or chloramphenicol. The inhibitory action of other antibiotics such as penicillin or erythromycin was not affected by addition of the test compound. The results suggest formation of a molecular complex between the azasteroid and antibiotic which is responsible for the enhanced biological activity. |
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Authors:
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R W Chesnut; N N Durham; R A Brown; E A Mawdsley; K D Berlin |
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Publication Detail:
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Type: Comparative Study; Journal Article; Research Support, U.S. Gov't, P.H.S. |
Journal Detail:
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Title: Steroids Volume: 27 ISSN: 0039-128X ISO Abbreviation: Steroids Publication Date: 1976 Apr |
Date Detail:
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Created Date: 1976-08-02 Completed Date: 1976-08-02 Revised Date: 2006-11-15 |
Medline Journal Info:
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Nlm Unique ID: 0404536 Medline TA: Steroids Country: UNITED STATES |
Other Details:
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Languages: eng Pagination: 525-41 Citation Subset: IM |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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Aminoisobutyric Acids
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metabolism Anti-Bacterial Agents* / pharmacology Azasteroids / pharmacology* Bacillus subtilis / drug effects* Drug Combinations Drug Resistance, Microbial Escherichia coli / drug effects* Glucose / metabolism Polymyxins / pharmacology* Protoplasts / drug effects Pseudomonas fluorescens / drug effects* Serine / metabolism Steroids, Heterocyclic / pharmacology* |
| Chemical | |
Reg. No./Substance:
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0/Aminoisobutyric Acids; 0/Anti-Bacterial Agents; 0/Azasteroids; 0/Drug Combinations; 0/Polymyxins; 0/Steroids, Heterocyclic; 50-99-7/Glucose; 56-45-1/Serine |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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