title: Synthesis, anticonvulsant and neurotoxicity screening of some novel 1,2,4-trisubstituted-1H-imidazole derivatives.
abstract: A series of 1,2,4-trisubstituted-1H- imidazole derivatives (4a-o) was synthesized by reacting 2,4-disubstituted-1H-imidazoles (3a-o) with chlorobenzene in the presence of triethylamine. Phenylglyoxal (2) was reacted with different aromatic aldehydes in the presence of ammonium acetate and glacial acetic acid to afford the disubstituted imidazoles (3a-o). The structures of the synthesized compounds were confirmed on the basis of their elemental analysis and spectral data results. Anticonvulsant activity was shown by majority of the synthesized compounds in the maximal electroshock (MES) and subcutaneous pentylenetetrazole (scPTZ) screens when given i.p. to mice. In anticonvulsant screening, only one compound 4k showed potent activity comparable to that of standard drugs phenytoin and carbamazepine. Compounds 4a, 4c, 4e, 41 and 4n passed the rotorod test successfully without any sign of neurological deficit.
authors.affiliation: Department of Pharmaceutical Chemistry, Jamia Hamdard University, Hamdard Nagar, New Delhi-1 10062, India. drasifhusain@yahoo.com
authors.forename: Asif
authors.initials: A
authors.lastname: Husain
authors.forename: Nadeem
authors.initials: N
authors.lastname: Siddiqui
authors.forename: Md
authors.initials: M
authors.lastname: Sarafroz
authors.forename: Yasmin
authors.initials: Y
authors.lastname: Khatoon
authors.forename: Mohd
authors.initials: M
authors.lastname: Rasid
authors.forename: Niyaz
authors.initials: N
authors.lastname: Ahmad
mesh_terms: D000818:Animals; D000927:Anticonvulsants / Q000138:chemical synthesis* / Q000494:pharmacology* / Q000633:toxicity; D004353:Drug Evaluation, Preclinical; D004597:Electroshock; D005260:Female; D007093:Imidazoles / Q000138:chemical synthesis* / Q000494:pharmacology* / Q000633:toxicity; D007202:Indicators and Reagents; D008297:Male; D051379:Mice; D020258:Neurotoxicity Syndromes / Q000473:pathology*; D010433:Pentylenetetrazole / Q000037:antagonists & inhibitors; D004856:Postural Balance / Q000187:drug effects; D012640:Seizures / Q000139:chemically induced / Q000517:prevention & control; D013329:Structure-Activity Relationship
chemical_list: D000927:Anticonvulsants; D007093:Imidazoles; D007202:Indicators and Reagents; D010433:Pentylenetetrazole