title: Synthesis and CNS depressant activity of some novel 3-[5-substituted 1,3,4-thiadiazole-2-yl]-2-styryl quinazoline-4(3H)-ones.
abstract: A series of novel 3-[5-substituted phenyl-1,3,4-thiadiazole-2-yl]-2-styryl quinazoline-4(3H)-ones were synthesized and evaluated for anticonvulsant, sedative-hypnotic and CNS depressant activities. After i.p. injection to mice at doses of 30, 100, and 300mg/kg body weight 2-styrylquinazolin-4(3H)-one derivatives were examined in the maximal electroshock induced seizures (MES) and subcutaneous pentylenetetrazole (scPTZ) induced seizure models in mice. The neurotoxicity was assessed using the rotorod method. Out of eighteen compounds only 4a, 4d, 4e, 4j and 4k showed anticonvulsant activity in one or more test models. All except 4e and 4f exhibited significant sedative-hypnotic activity via actophotometer screen. CNS depressant activity screened with the help of the forced swim pool method resulted into some potent compounds. From the experimental observation it can be concluded that synthesized compounds exhibited relatively better sedative-hypnotic and CNS depressant activities.
authors.affiliation: Pharmaceutical Chemistry Division, Department of Pharmaceutical Sciences, Dr. H.S.G. University, Sagar, M.P. 470003, India.
authors.forename: Varsha
authors.initials: V
authors.lastname: Jatav
authors.forename: Pradeep
authors.initials: P
authors.lastname: Mishra
authors.forename: Sushil
authors.initials: S
authors.lastname: Kashaw
authors.forename: J P
authors.initials: JP
authors.lastname: Stables
mesh_terms: D000818:Animals; D001522:Behavior, Animal / Q000187:drug effects; D002492:Central Nervous System Depressants / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D015195:Drug Design; D004597:Electroshock; D051379:Mice; D010433:Pentylenetetrazole / Q000037:antagonists & inhibitors; D052999:Quinazolinones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D051381:Rats; D013830:Thiadiazoles / Q000737:chemistry*
chemical_list: D002492:Central Nervous System Depressants; D052999:Quinazolinones; D013830:Thiadiazoles; D010433:Pentylenetetrazole