Source:http://linkedlifedata.com/resource/pubmed/id/12383016
Switch to
Predicate | Object |
---|---|
rdf:type | |
lifeskim:mentions | |
pubmed:issue |
22
|
pubmed:dateCreated |
2002-10-17
|
pubmed:abstractText |
Some new oxime ethers of types 7 and 8, in which the methyleneaminoxy group, C=N-O, of oxiconazole 6 is in an inverted atomic sequence, were synthesized and tested for their antifungal activities. Among them, the type 7 compounds, such as the N-ethoxy-morpholino-substituted derivatives 7l-o (Table 1), showed good antifungal properties against the Candida strains tested, with minimum inhibitory concentration (MIC) values similar to those of the reference drug 6. A remarkable result was obtained with these types of azoles, which had shown a cidal character against Candida albicans, while the reference drug oxiconazole was only fungistatic in the same tests. This fact may be seen from a comparison of the MIC values with those of the minimum fungicidal concentration (MFC) values for most of the type 7 compounds assayed that have shown differences between the MIC and the MFC, which are lower than three double diluitions. A simple molecular modeling of the P450 14-alpha-sterol demethylase from C. albicans (Candida P450DM) was built in order to understand how the structural differences between type 7 compounds and oxiconazole 6 can induce different antifungal profiles. The results of this work seem to confirm that it is possible to reverse the atomic sequence of the methyleneaminoxy group, C=N-O, of 6, obtaining new imidazoles possessing good antifungal properties.
|
pubmed:language |
eng
|
pubmed:journal | |
pubmed:citationSubset |
IM
|
pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Antifungal Agents,
http://linkedlifedata.com/resource/pubmed/chemical/Cytochrome P-450 Enzyme System,
http://linkedlifedata.com/resource/pubmed/chemical/Ethers,
http://linkedlifedata.com/resource/pubmed/chemical/Imidazoles,
http://linkedlifedata.com/resource/pubmed/chemical/Oxidoreductases,
http://linkedlifedata.com/resource/pubmed/chemical/Oximes,
http://linkedlifedata.com/resource/pubmed/chemical/Recombinant Fusion Proteins,
http://linkedlifedata.com/resource/pubmed/chemical/Sterol 14-Demethylase,
http://linkedlifedata.com/resource/pubmed/chemical/oxiconazole
|
pubmed:status |
MEDLINE
|
pubmed:month |
Oct
|
pubmed:issn |
0022-2623
|
pubmed:author | |
pubmed:issnType |
Print
|
pubmed:day |
24
|
pubmed:volume |
45
|
pubmed:owner |
NLM
|
pubmed:authorsComplete |
Y
|
pubmed:pagination |
4903-12
|
pubmed:dateRevised |
2010-11-18
|
pubmed:meshHeading |
pubmed-meshheading:12383016-Antifungal Agents,
pubmed-meshheading:12383016-Aspergillus fumigatus,
pubmed-meshheading:12383016-Candida,
pubmed-meshheading:12383016-Cryptococcus neoformans,
pubmed-meshheading:12383016-Cytochrome P-450 Enzyme System,
pubmed-meshheading:12383016-Ethers,
pubmed-meshheading:12383016-Imidazoles,
pubmed-meshheading:12383016-Microbial Sensitivity Tests,
pubmed-meshheading:12383016-Models, Molecular,
pubmed-meshheading:12383016-Oxidoreductases,
pubmed-meshheading:12383016-Oximes,
pubmed-meshheading:12383016-Recombinant Fusion Proteins,
pubmed-meshheading:12383016-Sterol 14-Demethylase,
pubmed-meshheading:12383016-Structure-Activity Relationship,
pubmed-meshheading:12383016-Trichophyton
|
pubmed:year |
2002
|
pubmed:articleTitle |
Synthesis, antifungal activity, and molecular modeling studies of new inverted oxime ethers of oxiconazole.
|
pubmed:affiliation |
Dipartimento di Scienze Farmaceutiche, Facoltà di Farmacia, Università degli Studi di Pisa, Via Bonanno, 6, 56100 Pisa, Italy.
|
pubmed:publicationType |
Journal Article
|