Synthesis, anticonvulsant and CNS depressant activity of some new bioactive 1-(4-substituted-phenyl)-3-(4-oxo-2-phenyl/ethyl-4H-quinazolin-3-yl)-urea.
Several new 1-(4-substituted-phenyl)-3-(4-oxo-2-phenyl/ethyl-4H-quinazolin-3-yl)-urea were synthesized and screened for anticonvulsant, CNS depressant and sedative-hypnotic activity in the mice. After i.p. injection to mice at doses of 30, 100, and 300 mg/kg body weight synthesized compounds were examined in the maximal electroshock induced seizures (MES) and subcutaneous pentylenetetrazole (scPTZ) induced seizure models in mice. Spectroscopic data and elemental analysis were consistent with the newly synthesized compounds. The neurotoxicity was assessed using the rotorod method. Compounds E1, E6, E9, E12, P3, P4 and P6 were found to be active in the MES screen whereas E1, P4, P6 and P11 were found to be active in the scPTZ screen. All except E6, E11 and P6 showed more than 50% decrease in locomotor activity at 1h of compound administration via actophotometer screen. CNS depressant activity screened with the help of the forced swim method resulted into some potent compounds. All the compounds were found to exhibit potent CNS depressants activity as indicated by increased immobility time. It can be concluded that newly synthesized compounds possessed promising CNS activities.
Kashaw
Sushil K
SK
Pharmaceutical Chemistry Division, Department of Pharmaceutical Sciences, Dr HS Gour University, Sagar 470003, India. sushilkashaw@gmail.com
Kashaw
Varsha
V
Mishra
Pradeep
P
Jain
N K
NK
Stables
J P
JP
D000818:Animals; D000927:Anticonvulsants / Q000138:chemical synthesis* / Q000737:chemistry / Q000627:therapeutic use*; D001522:Behavior, Animal / Q000187:drug effects; D002492:Central Nervous System Depressants / Q000138:chemical synthesis* / Q000737:chemistry / Q000627:therapeutic use*; D008297:Male; D051379:Mice; D015394:Molecular Structure; D010433:Pentylenetetrazole; D052999:Quinazolinones / Q000138:chemical synthesis* / Q000737:chemistry / Q000627:therapeutic use*; D051381:Rats; D017207:Rats, Sprague-Dawley; D017208:Rats, Wistar; D012640:Seizures / Q000139:chemically induced / Q000188:drug therapy*; D013329:Structure-Activity Relationship; D014508:Urea / Q000138:chemical synthesis / Q000737:chemistry / Q000627:therapeutic use
D000927:Anticonvulsants; D002492:Central Nervous System Depressants; D052999:Quinazolinones; D014508:Urea; D010433:Pentylenetetrazole