Synthesis and evaluation of 3-[(2,4-dioxo-1,3,8-triazaspiro[4.6]undec-3-yl)methyl]benzonitrile derivatives as potential anticonvulsants.
Arch Pharm (Weinheim)
; 346(3): 200-9, 2013 Mar.
Article
in En
| MEDLINE
| ID: mdl-23335463
ABSTRACT
New 3-[(2,4-dioxo-1,3,8-triazaspiro[4.6]undec-3-yl)methyl]benzonitrile derivatives 8-37 were synthesized and their pharmacological activities were determined with the objective to better understand their structure-activity relationship (SAR) for anticonvulsant activity. All the compounds were evaluated for their possible anticonvulsant activity by maximal electroshock seizure (MES) and pentylenetetrazole (PTZ) test. Compounds 11, 18, 31, and 32 showed significant and protective effect on seizure, when compared with the standard drug valproate. The same compounds were found to exhibit advanced anticonvulsant activity as well as lower neurotoxicity than the reference drug. From this study, it is quite apparent that there are at least three parameters for the activity of anticonvulsant drugs, that is, a lipophilic domain, a hydrophobic center, and a two-electron donor.
Full text:
1
Collection:
01-internacional
Database:
MEDLINE
Main subject:
Spiro Compounds
/
Drug Design
/
Anticonvulsants
/
Nitriles
Type of study:
Etiology_studies
Limits:
Animals
Language:
En
Journal:
Arch Pharm (Weinheim)
Year:
2013
Document type:
Article
Affiliation country:
India