一些新型喹喔啉衍生物作为抗惊厥剂的合成及生物学评价

Synthesis and biological evaluation of some novel quinoxaline derivatives as anticonvulsant agents.

作者信息

Elhelby Abdelghany Aly, Ayyad Rezk Rezk, Zayed Mohamed Fathalla

机构信息

Department of Pharmaceutical Chemistry, Faculty of Pharmacy (Boys), Al-Azhar University, Cairo, Egypt.

出版信息

Arzneimittelforschung. 2011;61(7):379-81. doi: 10.1055/s-0031-1296214.

DOI:10.1055/s-0031-1296214

PMID:21899204

Abstract

In view of their expected anticonvulsant activity, some new derivatives of quinonxaline (V1-7) were designed and synthesized by condensation of different aromatic aldehydes with 2-(2-oxo-3-phenylquinoxalin-1(2H)-yl)acetohydrazide (IV). All synthesized compounds were isolated and confirmed by IR, 1H-NMR, MS, elemental analysis and then tested as anticonvulsant agents. Compound V3 and V1 showed the highest anticonvulsant effect with anticonvulsant potency relative to phenobarbital sodium of 0.8 and 0.75 whereas compound V5 exhibited the lowest relative potency of 0.09. The other compounds showed variable activity between these values as follows: V2 = 0.19, V4 = 0.41, V6 = 0.1 and V7 = 0.15. All compounds showed less activity than the reference compound phenobarbital. But the compounds provided a basis for further optimization.

摘要

鉴于预期的抗惊厥活性，通过不同芳香醛与2-(2-氧代-3-苯基喹喔啉-1(2H)-基)乙酰肼(IV)缩合，设计并合成了一些新的喹喔啉衍生物(V1-7)。所有合成的化合物都经过分离，并通过红外光谱、1H-核磁共振、质谱、元素分析进行确认，然后作为抗惊厥剂进行测试。化合物V3和V1表现出最高的抗惊厥效果，相对于苯巴比妥钠的抗惊厥效力分别为0.8和0.75，而化合物V5表现出最低的相对效力，为0.09。其他化合物在这些值之间表现出不同的活性，如下所示：V2 = 0.19，V4 = 0.41，V6 = 0.1，V7 = 0.15。所有化合物的活性均低于参考化合物苯巴比妥。但这些化合物为进一步优化提供了基础。