Synthesis and Biological Screening of Novel Derivatives of Benzothiazol as Anticonvulsant Agents

Rachana B. Lamkane, Priyanka M. Khadasare, Pooja M. Shinde, T. P. Yele, Amarja B. Mohite, Priyanka B. Parekar, Shivraj S. Shivpuje
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Abstract

The Benzothiazole ring system belongs to a much studied class of compound. In the last few decades, the chemistry of benzothiazole and their fused heterocyclic derivatives have received considerable attention owing to their significant and effective biological activity. The present study aimed to design and synthesize novel derivatives of bezothiazole obtained from 3-chloro-4-flouro aniline treated with potassium thiocynide with chloro acetyl chloride gives (7-chloro-6-fluro-1,3-benzothiazol-2-yl) acetyl chloride which is converted into hydrazide and yields the resultant compound derivatives of 2-(7-chloro-6-fluro-1,3-benzothiazol-2-yl) –N’-[(Z)-phenyl methylidene] acetohydrazide (SMVB-IIIA-IIIG).Title compound were synthesized and the structures of newly synthesized compounds were confirmed by IR, Mass and 1H-NMR spectroscopy All the compounds synthesized were confirmed by spectral data and evaluated for their anticonvulsant activity. The Compounds SMVB-IIIC, SMVB-IIIEand SMVB-IIIF showed maximal activity whereas remaining compounds showed good activity.
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新型苯并噻唑类抗惊厥药物的合成及生物学筛选
苯并噻唑环系是一类研究较多的化合物。近几十年来,苯并噻唑及其融合杂环衍生物因其显著而有效的生物活性而受到广泛关注。以3-氯-4-氟苯胺为原料,经硫辛酸钾和氯乙酰氯处理,得到(7-氯-6-氟-1,3-苯并噻唑-2-基)乙酰氯,乙酰氯转化为肼,得到2-(7-氯-6-氟-1,3-苯并噻唑-2-基)- n′-[(Z)苯基甲基]乙酰肼(smbb - iiia - iiig)。合成了标题化合物,并对新合成化合物的结构进行了IR、Mass和1H-NMR鉴定。所有合成的化合物均经光谱数据证实,并评价了其抗惊厥活性。化合物SMVB-IIIC、smvb - iiie和SMVB-IIIF活性最高,其余化合物活性较好。
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