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| Format: | Recurso digital |
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Zenodo
2025
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| Accès en ligne: | https://doi.org/10.5281/zenodo.17277591 |
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- <p><span>One of the most common methods for the synthesis of 1,5-¬ benzothiazepines is based on condensation reaction of o-aminothiophenol with chalcones under acidic or basic media [1]. The synthesis of compounds 1a–1g (Scheme 1) was performed in three steps. compound 3 P-Hydroxy aromatic aldehydes were condensed with 2,4- pentandione in dry benzene using piperidine as a catalyst to yield compound 3. And then the Michael addition of o-aminothiophenol to compound 3, gave 4-substituted pentandione derivatives 4. The intramolecular cyclisation of 4 followed by dehydration in acetic acid/methanol finally gave compounds 1, which were purified by crystallization from dry methanol. The synthesized new compounds were identified on the basis of their elemental analysis, IR and 1HNMR and Mass etc. The synthesized compounds were evaluated for their in-vitro antimicrobial activities against the three bacterial strains C. albicans, S. aureus, S. epidermidis by using disk diffusion method. Some of the title compounds exhibited significant activity as compared to Fluconazole a reference drug.</span></p>