This research includes synthesis of new heterocyclic derivatives of disubstituted 1,3-oxazepine-5-one. Azomethine compounds (N1-N5) were synthesized by the reaction of aromatic aldehydes with primary aromatic amines, in the presence of glacial acetic acid as a catalyst in absolute ethanol. The synthesized compounds were identified via spectral methods viz., FT-IR, 1H-NMR, and 13C-NMR and measurements of some physical properties. The prepared oxazepine compounds (N6-N10) were obtained from treatment of azomethine compounds with phthalide. N9 and N7 derivatives have recorded the higher zone of inhibition 15 mm against Candida guilliermondii and Candida zeylanoides respectively. The lower zone of inhibition was 8.0 mm and 9.3 mm by N7 toward the growth of Candida albicans and Candida guilliermondii respectively. Slight variation in the structure of those derivatives can show the very dramatic effect on the efficiency of these compounds in their bio-activity and may be helpful in designing more antifungal agents for therapeutic use in future.
Novel 1,3-oxazepine derivatives have been synthesis via (2+5) cycloaddition reaction of imines and selected cyclic carboxylic acid anhydrides by refluxing in dry benzene. Imines have been prepared by thermal condensation of 4-methyl aniline and para substituted benzaldehyde in absolute ethanol under reflux conditions. The structure of the target compounds were Identified by some physical properties and spectral data of FT-IR and 1H-NMR.
Some new tetrazole derivatives were prepared by the reaction between the prepared azomethine compounds I 6-I 10 with sodium azide in anhydrous tetrahydrofuran (THF) with a few drops of distilled water and under reflux conditions. Azomethine compounds were prepared by thermal condensation reactions of aromatic aldehydes with primary aromatic amines. The prepared compounds (tetrazole derivatives) were screened for their antibacterial activity (by disc diffusion method). Compound I 6 is the most active derivative that has recorded a significantly (p<0.01) stronger influence to inhibit the growth of Candida zeylanoides with an average zone of inhibition of 26.0 mm. Derivatives I 7 and I 9 showed the lowest zone of inhibition of 8.0 mm against Candida zeylanoides. This study may be helpful in designing more potential anticandidal agents for therapeutic use in the future.
This research includes synthesis of new heterocycles containing disubstituted Tetrazole derivatives. Imine compounds were synthesized by reaction of primary aromatic amines with various substituted benzaldehydes in the presence of glacial acetic acid as catalyst in absolute ethanol to obtain new imine compounds O 1-O 5. The novel five-membered heterocycles as Tetrazole derivatives O 6-O 10 were obtained from treatment of each new imine compounds with sodium azide compound. Newly synthesized compounds were identified via spectral methods (FT-IR, 1 H-NMR and 13 C-NMR) spectra and some physical properties. O 6 is the best derivative that has significantly (p<0.01) recorded a stronger influence to inhibit the growth of Candida guilliermondii at an average of the zone of inhibition 14.0 mm. While, O 9 derivative recorded the lowest zone of inhibition 7.3 mm toward the same clinical fungal pathogen. The present work may be helpful in designing more potential antibacterial and antifungal agents for therapeutic use in the future.
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