PHARMACOLOGICAL EVALUATION OF SOME 1-(SUBSTITUTEDBENZYLIDENE)-4-(4-(2-(METHYL/PHENYL)-4-OXOQUINAZOLIN-3(4H)-YL)PHENYL)SEMICARBAZIDE DERIVATIVES


Govindaraj Saravanan, Veerachamy Alagarsamy

ABSTRACT
A series of 1-(substitutedbenzylidene)-4-(4-(2-(methyl/phenyl)-4-oxoquinazolin- 3(4H)-yl)phenyl) semicarbazide derivatives were synthesized and evaluated for analgesic, anti-inflammatory and ulcerogenic activities. The title compounds were screened for analgesic activity by tail‒flick technique using Wistar albino mice orally at two dose levels i.e. 10 and 20 mg/kg. The carrageenan-induced foot paw edema test was performed for screening anti-inflammatory activity of title compounds orally at two dose levels i.e. 10 and 20 mg/kg in rats. Diclofenac sodium at 10 and 20 mg/kg was administered orally as reference drug for comparison. In addition all compounds were examined for its ulcerogenicity. Results revealed that entire series of compounds exhibited mild to excellent analgesic and anti-inflammatory activity with low to moderate ulcer index. The reports indicate that all the test compounds exhibited significant activity and graded dose response. Moreover this study revealed that test compounds showed moderate analgesic and anti-inflammatory activity at 30 min of reaction time; the activity increased at 1 h, further it reached to peak level at 2 h and past its best in activity was observed at 3 h. The relationship between the functional group variation and the biological activity of the evaluated compounds were well discussed. From the results in general, it was observed that 2-phenyl quinazolinone analog exhibited better activity than corresponding 2-methyl quinazolinone analog. Based on the results obtained, compound 5k and 5m was found to be very active with low ulcer index compared to the rest of the compounds which were tested.
KEY WORDS : Quinazolin-4(3H)-one, Analgesic, Anti-inflammatory and Semicarbazide.