Structure Activity Relationship Studies of Synthesized Diamides on CNS Depression and Sleeping Time Potentiation Effect

Evaluation of structure activity relationship studies of synthesized diamides on CNS depression and sleeping time potentiation effect through intraperitoneally administration of various doses of test compounds in mg/kg dose in group of male albino mice using propylene glycol as an inert vehicle. The loss of righting reflex and regaining of it was noted for each compounds to determine the sleeping time, injecting drug (diazepam/pentobarbitone) solution to mice, compound+drug solution in the mice and only compound solution to another mice and observed it's sleeping time potentiation and by plotting the histogram sleeping time has been observed. It has been found that all the teat compounds do not have sleep inducing property. Sleeping time potentiation effect was studied for the teat compounds by using diazepam as benzodiazepine series and pentobarbitone as barbiturate series which show good sleep inducing property. The amide groups of compounds block the GABA receptor and chloride channel and shows longer duration of sleep inducing properrty due to the presence of two amide linkages on male albino mice. Maximum activity was shown by Compound-93 (b) due to the presence of two free -CONH2 linkages and also show more lipid solubility which block GABA receptor ling time produce their effect for longer period of time.
All the compounds exhibited significant CNS depression activity in combination with standard drug diazepam and pentobarbitone.