Synthesis and Evaluation of Antipsychotic and Anticonvulsant Activity of Indol-5-YL and Benzoxazepin-4-YL Carbazoles

Archana., A. Sindhu
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Abstract

Various1-(substituted indolylidenylchalconyl) carbazole(2a-2b), 1-[2-(5substituted indolyl)-1 ’ , 5 ’ -benzoxazepinyl]-carbazoles(3a-3b) and 1-[2 ’ -(5 ’’ -substituted indolyl)-3’-(2’’’-substitutedphenyl amino)-methyl-1’, 5 ’ -benzoxazepinyl]-carbazoles(4a-4n) have been synthesized according to scheme -1. These compounds were screened for antipsychotic and anticonvulsant activity as well as for acute toxicity. Compound 4dI.E. 1-[2 ’ (5 ’’ -methoxy indolyl)-3’-(2’’’,3’’’dichlorophenyl amino)-methyl-1’, 5 ’ -benzoxazepinyl]carbazoles showed most promising antipsyctotic and anticonvulsant activity with ALD50greaterthan 2000 mg/kg i.p. The structures of all the newly synthesized compounds were confirmed by elemental (C, H, N) and spectral (IR, 1 H-NMR and mass) analysis.
吲哚-5-酰基和苯并恶西平-4-酰基咔唑的合成及抗精神病和抗惊厥活性评价
根据方案-1合成了各种1-(取代吲哚基查尔基)咔唑(2a-2b)、1-[2-(5取代吲哚基)-1 ',5 ' -苯并恶唑基]-咔唑(3a-3b)和1-[2 ' -(5 ' -取代吲哚基)-3 ' -(2 ' ' -取代苯基氨基)-甲基-1 ',5 ' -苯并恶唑基]-咔唑(4a-4n)。筛选了这些化合物的抗精神病和抗惊厥活性以及急性毒性。化合物4 di.e。1-[2 '(5 ' -甲氧基吲哚基)-3 ' -(2 ',3 ' '二氯苯基氨基)-甲基-1 ',5 ' -苯并恶唑基]咔唑类化合物具有抗精神病和抗惊厥活性,其抗精神病和抗惊厥活性均大于2000 mg/kg。所有新合成化合物的结构均通过元素(C, H, N)和光谱(IR, 1h - nmr和质量)分析得到证实。
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