Synthesis and anti-inflammatory activity of newer quinazolin-4-one derivatives.
2-Methyl-3-aminosubstituted-3H-quinazolin-4-ones (1-2), 2-methyl-3-(substituted-arylidene-amino)-substituted-3H-quinazolin-4-ones (3-10), 2-bromomethyl-3-(substituted-arylidene-amino)-substituted-3H-quinazolin-4-ones (11-18), 2-(5'-pyridin-4-yl-[1,3,4]-oxadiazol-2-yl-sulfanylmethyl)-3-(substituted-arylidene-amino)-substituted-3H-quinazolin-4-ones (19-26), 3-(3-chloro-2-oxo-4-substituted-aryl-azetidin-1-yl)-2-(5-pyridin-4-yl-[1,3,4]-oxadiazol-2-yl-sulfanylmethyl)-substituted-3H-quinazolin-4-ones (27-34) and 3-(4-oxo-2-substituted-aryl-thiazolidin-3-yl)-2-(5-pyridin-4-yl-[1,3,4]-oxadiazol-2-yl-sulfanylmethyl)-substituted-3H-quinazolin-4-ones (35-42) were synthesized in present study. All the compounds exhibited anti-inflammatory activity at the dose 50 mg/kg p.o. varying degree from 16.3 to 36.3% inhibition of oedema. Compound 40 showed same activity at 25, 50 and 100 mg/kg p.o. like standard drugs. The structure of all these newly synthesized compounds was confirmed by their analytical (C, H, N) and spectral (IR and (1)H NMR) data.
Kumar
Ashok
A
Medicinal Chemistry Division, Department of Pharmacology, L.L.R.M. Medical College, Gargh Road, Meerut, U.P. 250004, India. rajputak@gmail.com
Rajput
Chatrasal Singh
CS
D000818:Animals; D000893:Anti-Inflammatory Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D004305:Dose-Response Relationship, Drug; D004487:Edema / Q000188:drug therapy / Q000517:prevention & control; D015394:Molecular Structure; D052999:Quinazolinones / Q000138:chemical synthesis* / Q000494:pharmacology; D051381:Rats; D013057:Spectrum Analysis
D000893:Anti-Inflammatory Agents; D052999:Quinazolinones