title: Synthesis and anticonvulsant activity of some 2-(2-{1-[substituted phenyl]ethylidene}hydrazinyl)-4-(4-methoxy-phenyl)-6-oxo-1,6-dihydro-pyrimidine-5-carbonitrile.
abstract: A series of dihydro-pyrimidine-5-carbonitrile derivatives (3-16) were synthesized and evaluated for their anticonvulsant activity against MES and scPTZ models. Motor impairment screening was carried out by rotarod test method and CNS depressant effect was determined by Porsolt's force swim pool method. Compounds 4 and 9 having p-substituted bromo and m-substituted nitro groups, respectively, were found to be most active showing activity both in MES and scPTZ screen at lower doses of 30 mgkg(-1) at 0.5 h and 100 mgkg(-1) at 4 h. In the rotarod motor impairment screen, compound 4 did not show any motor impairment even at the maximum dose of 300 mgkg(-1); however, compound 9 showed motor impairment at 300 mgkg(-1) dose after 4.0 h. The compounds were also tested for their CNS depression effect. The compounds 4 and 9 showed 41.38 and 43.44% increase in immobility time with respect to control. The pharmacophore hypothesis also fits best for compounds 4 and 9.
authors: Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Hamdard University, New Delhi, India. shaqiq@gmail.com
authors: Mohammad
authors: M
authors: Shaquiquzzaman
authors: Suroor Ahmad
authors: SA
authors: Khan
authors: Mohammad
authors: M
authors: Amir
authors: Mohammad Mumtaz
authors: MM
authors: Alam
mesh_terms: D000818:Animals; D000927:Anticonvulsants / Q000138:chemical synthesis* / Q000494:pharmacology; D001522:Behavior, Animal / Q000187:drug effects; D002492:Central Nervous System Depressants / Q000138:chemical synthesis* / Q000494:pharmacology; D003292:Convulsants; D004195:Disease Models, Animal; D004305:Dose-Response Relationship, Drug; D004597:Electroshock; D005260:Female; D006834:Hydrazines / Q000138:chemical synthesis* / Q000494:pharmacology; D008297:Male; D051379:Mice; D009570:Nitriles / Q000138:chemical synthesis* / Q000494:pharmacology; D010433:Pentylenetetrazole; D011743:Pyrimidines / Q000138:chemical synthesis* / Q000494:pharmacology; D045442:Rotarod Performance Test; D012640:Seizures / Q000139:chemically induced / Q000188:drug therapy* / Q000503:physiopathology; D013329:Structure-Activity Relationship
chemical_list: D000927:Anticonvulsants; D002492:Central Nervous System Depressants; D003292:Convulsants; D006834:Hydrazines; D009570:Nitriles; D011743:Pyrimidines; D010433:Pentylenetetrazole