Synthesis of Novel Indolylbenzothiazepines/ Indolylbenzoxaziepines Substituted 2-Oxo/Thiobarbituric acids as Potential Anticonvulsant Agents

被引:0
作者
Archana [1 ]
Awasthi, Abha [1 ]
Chaudhary, Sakshi [2 ]
机构
[1] Meerut Univ, Dept Chem, Med Chem Lab, Meerut 250002, UP, India
[2] DNPG Coll, Dept Chem, Meerut 250002, UP, India
关键词
Benzothiazepines; Benzoxazepines; indoles; oxo/thiobarbituric acid; synthesis; antiepileptic activity; ALD50; BENZOXAZEPINE DERIVATIVES;
D O I
10.13005/ojc/400129
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
4-(2'-Oxo/thiobarbiturinyl acid)-2-(2"-halo-1"H-indolyl)-2,3-dihydro--1,5-benzothiazepines (7-10) and 4-(2'-oxo/thiobarbiturinyl acid)-2-(2"-halo-1"H-indolyl)-2,3-dihydro--1,5-benzoxazepines (11-14) undergoes Mannich reaction to afford compounds 4-(2'-oxo/thiobarbiturinyl acid)-2-(2"halo-1"H-indolyl)-3-(substitutedphenyl aminomethylene)-2,3-dihydro-1,5-benzothiazepines (15-22) and 4-(2'-oxo/thiobarbiturinyl acid)-2-(2"-halo-1"H-indolyl)-3-( substitutedphenyl aminomethylene)2,3-dihydro-1,5-benzoxazepines (23-30) correspondingly. All the chemical framework of these newer drugs were elucidated by using elemental and IR and NMR spectroscopy. All these newly synthesized compounds were tested for antiepileptic effect against SMES experimental models and the results were collated with phenytoin sodium-standard drug. Results of antiepileptic profile showed promising effect in most of the derivatives synthesized. Activity equal to standard drug was shown by compounds 9 and 28. The most promising and active compound of this project was found to be 4-(2'- thiobarbiturinyl acid)-2-(2"-chloro-1"H-indolyl)-3-(chlorophenyl aminomethylene)-2,3-dihydro1,5-benzothiazepines, which elicited activity greater than the standard drug. All the antiepileptic drugs of the produced in this projects were also tested for ALD50.
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收藏
页码:239 / 246
页数:8
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