1-4-benzothiazine and Candidiasis

1-4-benzothiazine has been researched along with Candidiasis* in 1 studies

Other Studies

1 other study(ies) available for 1-4-benzothiazine and Candidiasis

Article	Year
Novel ketoconazole analogues based on the replacement of 2,4-dichlorophenyl group with 1,4-benzothiazine moiety: design, synthesis, and microbiological evaluation. Bioorganic & medicinal chemistry, 2006, Aug-01, Volume: 14, Issue:15 As a part of a program to develop novel antifungal agents, new compounds which incorporate the 1,4-benzothiazine moiety into the structure of ketoconazole (KTZ) were prepared. These compounds were computationally investigated to assess whether the 1,4-benzothiazine moiety was a suitable bioisosteric replacement for the 2,4-dichlorophenyl group of KTZ in order to obtain a more potent inhibition of CYP51 enzyme of Candida albicans. Results of preliminary microbiological studies show that the racemic cis-7 analogue has a good in vivo activity, comparable to that of KTZ, but the best activity was observed in the racemic trans-7 analogue. Topics: Animals; Candida albicans; Candidiasis; Crystallography, X-Ray; Cytochrome P-450 Enzyme Inhibitors; Cytochrome P-450 Enzyme System; Disease Models, Animal; Enzyme Inhibitors; Female; Fungal Proteins; Hydrocarbons, Chlorinated; Immunologic Tests; Ketoconazole; Kidney; Mice; Microbial Sensitivity Tests; Models, Molecular; Molecular Structure; Stereoisomerism; Structure-Activity Relationship; Thiazines	2006

Article

Year

Novel ketoconazole analogues based on the replacement of 2,4-dichlorophenyl group with 1,4-benzothiazine moiety: design, synthesis, and microbiological evaluation.

Bioorganic & medicinal chemistry, 2006, Aug-01, Volume: 14, Issue:15

As a part of a program to develop novel antifungal agents, new compounds which incorporate the 1,4-benzothiazine moiety into the structure of ketoconazole (KTZ) were prepared. These compounds were computationally investigated to assess whether the 1,4-benzothiazine moiety was a suitable bioisosteric replacement for the 2,4-dichlorophenyl group of KTZ in order to obtain a more potent inhibition of CYP51 enzyme of Candida albicans. Results of preliminary microbiological studies show that the racemic cis-7 analogue has a good in vivo activity, comparable to that of KTZ, but the best activity was observed in the racemic trans-7 analogue.

Topics: Animals; Candida albicans; Candidiasis; Crystallography, X-Ray; Cytochrome P-450 Enzyme Inhibitors; Cytochrome P-450 Enzyme System; Disease Models, Animal; Enzyme Inhibitors; Female; Fungal Proteins; Hydrocarbons, Chlorinated; Immunologic Tests; Ketoconazole; Kidney; Mice; Microbial Sensitivity Tests; Models, Molecular; Molecular Structure; Stereoisomerism; Structure-Activity Relationship; Thiazines

2006