1382229-29-9Relevant academic research and scientific papers
New quinazolinone-pyrimidine hybrids: Synthesis, anti-inflammatory, and ulcerogenicity studies
Abbas, Safinaz E.,Awadallah, Fadi M.,Ibrahin, Nashwa A.,Said, Eman G.,Kamel, Gihan M.
, p. 141 - 149 (2012/08/08)
Two groups of hybrid compounds: the quinazolinone-dihydropyrimidines and quinazolinone-pyrimidines, were synthesized. The starting derivative 3 was reacted with chloroacetyl chloride to give intermediate 5 which was condensed with the 2-mercaptopyrimidines 4a-c affording compounds 6a-c. These latter compounds underwent hydrolysis and N-alkylation reactions to give the dihydropyrimidine derivatives 7a-c and 8a-f, respectively. The chloro derivatives 9a-c subsequently reacted with various anilines furnishing compounds 10a-i. The anti-inflammatory activity of the synthesized compounds were evaluated using the carrageenan-induced rat paw oedema model and ulcer indices for the most active compounds were calculated. Five compounds were found more active and less ulcerogenic than diclofenac particularly compound 10g (IC 50 = 116.73 μmol/kg; ulcer index = 11.38). Compound 10g was also 2-fold more selective inhibitor of COX-2 than COX-1.
