Design, synthesis and anticonvulsant activities of novel 1-(substituted/unsubstituted benzylidene)-4-(4-(6,8-dibromo-2-(methyl/phenyl)-4-oxoquinazolin-3(4H)-yl)phenyl) semicarbazide derivatives.

Abstract:

:Novel quinazolinone derivatives 5a-5n were designed, synthesized and screened for antiepileptic activity using MES and scPTZ seizures tests. Neurotoxicity study was performed by rotorod test. Compounds 5c, 5d, 5g, 5j and 5k were found active in the preliminary screening in MES model and/or scPTZ model. Further all these five compounds were administered to rats, 5c and 5d showed better activity than Phenytoin in oral route. Among all the title compounds tested, the most active one was 5c that revealed protection in MES at a dose of 30 mg/kg (ip) after 0.5 and 4h. This molecule also provided protection in the scPTZ at a dose of 100mg/kg (0.5h) and 300 mg/kg (4h).

journal_name

Bioorg Med Chem Lett

authors

Saravanan G,Alagarsamy V,Prakash CR

doi

10.1016/j.bmcl.2012.03.068

subject

Has Abstract

pub_date

2012-05-01 00:00:00

pages

3072-8

issue

9

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(12)00389-7

journal_volume

22

pub_type

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