Synthesis and Biological Activity Evaluation of Some New Coumarin Derivatives as Potent Anticonvulsant and CNS-Depressant Agents

نویسندگان

چکیده

Triazolo-thiadiazines 4a–f and triazolo-tetrazines 8g–l were prepared from reaction of 3-(4-amino-5-mercapto-4H-1,2,4-triazol-3-yl)-2H-chromen-2-one with the respective hydrazonoyl halides 2a–f 2g–l. Moreover, aminomercaptotriazole derivative phenacyl bromide ethyl 2-chloro-3-oxobutanoate followed by coupling products benzenediazonium chloride yielded corresponding 4f 8g, respectively. All newly heterocyclic derivatives determined using spectral data, elemental analysis, alternate methods. The in-vivo anticonvulsant CNS-depressant activities all tested maximal electroshock method showed excellent activities, especially triazolo[4,3-b]tetrazine 8j, 8k, 8l. Additionally, their structure–activity relationship was proven clearly, demonstrating that electron-releasing groups increase while electron-withdrawing lower them.

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ژورنال

عنوان ژورنال: Polycyclic Aromatic Compounds

سال: 2022

ISSN: ['1563-5333', '1026-7743', '1040-6638']

DOI: https://doi.org/10.1080/10406638.2022.2050268