Synthesis and Pharmacological Evaluation of Novel 1'-[2-(Difluoromethoxy)benzyl]-2'H,5'H-spiro[8-azabicyclo[3.2.1]-octane-3,4'-imidazolidine]-2',5'-diones and Their Derivatives

被引：28

作者：

Madaiah, Malavalli ^{[1
]}

Prashanth, Maralekere K. ^{[1
]}

Revanasiddappa, Hosakere D. ^{[1
]}

Veeresh, Bantal ^{[2
]}

机构：

[1] Univ Mysore, Dept Chem, Mysore 570006, Karnataka, India

[2] G Pullareddy Coll Pharm, Dept Pharmacol, Hyderabad, Andhra Pradesh, India

来源：

ARCHIV DER PHARMAZIE | 2014年 / 347卷 / 05期

关键词：

Anticonvulsant; Isocyanate; Maximal electroshock; ScPTZ; Spirohydantoins; ANTIEPILEPTIC DRUG DEVELOPMENT; ANTICONVULSANT ACTIVITIES; HYDANTOINS; DISCOVERY; BINDING; SERIES;

D O I：

10.1002/ardp.201300289

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of novel 1-[2-(difluoromethoxy)benzyl]-2H,5H-spiro[8-azabicyclo[3.2.1]octane-3,4-imidazolidine]-2,5-dione substituted hydantoins (5-32) were synthesized using an appropriate synthetic route and characterized by elemental analysis and spectral data. The novel molecules were screened for anticonvulsant activity in mice by maximal electroshock (MES) and subcutaneous pentylenetetrazol (ScPTZ)-induced seizure tests. The neurotoxicity was assessed using the rotarod method. Compounds 9, 10, 18, 30, and 31 exhibited anticonvulsant potency against MES seizure and in the ScPTZ model, with lesser neurotoxicity. Some title compounds showed lesser central nervous system depression compared to phenytoin.

引用

页码：370 / 380

页数：11

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