A series of new hybrid benzothiazole containing pyridazinones derivatives were designed and synthesized fulfilling all the pharmacophoric requirements essential for the anticonvulsant activity. In-silico and in vitro studies revealed that some of these hybrid derivatives demonstrated admirable GABA AT inhibitory activity. An attempt has also been made to validate the results of in vitro GABA AT inhibition of the most potent compound SPS-5F (IC₅₀ 9.10 μM) through in vivo anticonvulsant screening. Compound SPS-5F administration significantly increases the whole brain GABA level, might be through the inhibition of GABA AT enzyme.

中文翻译：

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哒嗪酮杂化物：设计，合成和评估为潜在的抗惊厥药

设计并合成了一系列新的含有哒嗪酮衍生物的杂苯并噻唑杂化物，以满足抗惊厥活性必不可少的所有药理学要求。硅和体外研究表明，这些杂化衍生物中的一些表现出令人钦佩的GABA AT抑制活性。还尝试通过体内抗惊厥筛选来验证体外GABA AT抑制最有效化合物SPS-5F（IC ₅₀ 9.10μM）的结果。化合物SPS-5F的给药可显着增加全脑GABA水平，可能是通过抑制GABA AT酶。