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Biomedical subjects

J T Mitchell

Publications and source records attributed to J T Mitchell.

At least 37 records · Page 2Linked to original sources
PubMed1988

5-( [aryl or aryloxy (or thio)]methyl)-3-(1H-imidazol-1-ylmethyl)-3- (2-thienyl)-2-methylisoxazolidine derivatives as novel antifungal agents.

The in vitro antifungal activity of a novel series of cis- and trans-5-([aryl or aryloxy (or thio)]methyl)-3-(1H-imidazol-1-ylmethyl)-3- (2-thienyl)-2-methylisoxazolidines (13-24) was evaluated and compared with ketoconazole. The title series of compounds was prepared via a 1,3-dipolar cycloaddition reaction of 1-(2-thienyl)-2-(1H-imidazol-1-yl)-N-methylethanimine N-oxides with appropriate styrenes, allyl phenyl ethers, or allyl phenyl thioether precursors. The resulting products were mixtures of the corresponding cis- and trans-diastereomers which were readily separated by flash chromatography on neutral silica gel. The majority of compounds 13-24, when tested in solid agar cultures, exhibited moderate to potent activity against Trichophyton rubrum, Aspergillus fumigatus, and Candida albicans at concentrations ranging between less than or equal to 2.0 and 70.0 micrograms/mL.

Antifungal Agents↗
PubMed1988

Studies on antifungal agents. 23. Novel substituted 3,5-diphenyl-3-(1H-imidazol-1-ylmethyl)- 2-alkylisoxazolidine derivatives.

The synthesis and antifungal activity of a novel series of substituted 3,5-diphenyl-3-(1H-imidazol-1-ylmethyl)-2-alkylisoxazolidine derivatives (15-30) are described. The synthesis of the title compounds was accomplished via a 1,3-dipolar cycloaddition reaction of alpha-substituted ketonitrones with appropriate styrene precursors. The compounds when tested in vitro in solid agar cultures exerted a very potent antifungal activity against a wide variety of yeast and systemic mycoses and dermatophytes, especially Trichophyton and Microsporum sp., Epidermophyton floccosum and Candida stellatoidea. The in vitro activity against Aspergillus fumigatus and Candida albicans was moderate to potent. Overall, the two bis(4-chlorophenyl) analogues 18 and 19 were the most potent in vitro compounds, showing MIC values ranging between 0.2 and 7.0 microgram/mL, as compared to 0.2-20.0 micrograms/mL for ketoconazole, which was used as the positive standard in all assays. When tested in vivo in the rat vaginal candidiasis model, derivative 18, although showing significant antifungal activity when compared to controls, was less effective than ketoconazole. The title 3,5-substituted isoxazolidine compounds represent a novel class of potent antifungal agents.

Animals↗
PubMed1988

Studies on antifungal agents. 17. Effects of the C-5-substitution on the in vitro activity of novel 3,5-substituted isoxazolidines.

A number of novel 5-(substituted thiomethyl)-3-phenyl-3-(1H-imidazol-1-ylmethyl)-2- methylisoxazolidine derivatives were prepared and evaluated in vitro for antifungal activity in solid agar cultures against Trichophyton rubrum, Aspergillus fumigatus and Candida albicans. The effect of the 5-(substituted thiomethyl) group on the degree and scope of activity was studied and compared to that of the corresponding 5-phenoxymethyl and 5-[(substituted phenyl)thio(or amino)methyl] derivatives.

Antifungal Agents↗
PubMed1988

Studies on antifungal agents. 18. In vitro activity of 5,5-disubstituted-3-phenyl-3-(1H-imidazol-1-ylmethyl)-2-methy lisoxazol idines and related compounds.

The in vitro antifungal activity of a series of novel 5,5-disubstituted-3-phenyl-3-(1H-imidazol-1-ylmethyl)-2-methyli soxazolidines and related compounds against Trichophyton rubrum, Aspergillus fumigatus and Candida albicans was studied. The screening was performed in solid agar cultures and some structure-activity relationships involving the C-5-substitution pattern are discussed.

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