A series of novel 2-phenyl-3-substituted quinazolin-4(3H)-ones have been synthesized by treating methyl-N-(2-phenyl quinazolin-3-yl-4(3H)-one) dithiocarbamate with different amines, the starting material dithiocarbamate was synthesized from anthranilic acid. The title compounds were investigated for analgesic, anti-inflammatory and antibacterial activities. All the test compounds exhibited significant activity, the compounds A1, A2 and A3 shown more potent analgesic activity, and the compound A3 shown more potent anti-inflammatory activity than the reference standard diclofenac sodium.
A series of 2-Substituted (1,3,4) thiadiazolo quinazolines were synthesized by the cyclocondensation of 3-amino-2-mercapto quinazolin-4(3H)-ones with various one-carbon donors and screened for their CNS activities (analgesic, anti-inflammatory, sedative-hypnotic and anticonvulsant). Compound III showed good CNS depressant activity, and it is comparable with the reference standard diazepam. While all the test compounds offered significant protection against strychnine-induced and hypoxic induced convulsion, compound III exhibited equivalent activity with the standard diazepam at the dose tested, and it was found to be significant when compared to control.
A variety of novel 3-propyl-2-substitutedamino-quinazolin-4(3H)-ones were synthesized by reacting the amino group of 2-hydrazino-3-propyl quinazolin-4(3H)-one with a variety of aldehydes and ketones. The starting material 2-hydrazino-3-propyl quinazolin-4(3H)-one was synthesized from propylamine. The title compounds were investigated for analgesic and anti-inflammatory activities. The compound 2-(1-ethylpropylidene-hydrazino)-3-propyl-quinazolin-4(3H)-one (SR2) emerged as the most active compound of the series, and it is more potent in its analgesic and anti-inflammatory activities when compared with the reference standard diclofenac sodium. NS, Not significant. Data expressed as mean AE standard error of the mean from six different experiments carried out in duplicate. Significance levels a p < 0.05, b p < 0.01, and c p < 0.001 as compared with the respective control.
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Purpose: To synthesize a series of novel 3-ethyl-2-substituted amino-quinazolin-4(3H)-ones and evaluate them for their analgesic and anti-inflammatory activities.
Methods: The compounds, 3-ethyl-2-substituted amino-quinazolin-4(3H)-ones, were synthesized by reacting the amino group of 3-ethyl-2-hydrazino quinazolin-4(3H)-one with a variety of aldehydes and ketones. The synthesized compounds were characterized by Fourier transform infrared (FTIR), protonnuclear magnetic resonance spectroscopy ( 1 H-NMR) and mass spectrometry. The purity of the compounds was determined by elemental analysis. Test for analgesic activity was performed by tail-flick technique using Wistar albino mice while anti-inflammatory activity was evaluated by carrageenaninduced paw oedema test in rats. Diclofenac sodium was used as positive control for both analgesic and anti-inflammatory activities.
Results: The compound, 3-ethyl-2-(cyclohexylidene-hydrazino)-3H-quinazolin-4-one (AS1), emerged as the active analgesic (activity, 63.89 %) and anti-inflammatory (activity, 60.00 %)
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