Analgesic, anti-pyretic and DNA cleavage studies of novel pyrimidine derivatives of coumarin moiety

A novel series of 4-[4-(6-phenyl-pyrimidin-4-yl)-phenoxymethyl]-chromen-2-ones [5–7(a–e)] were synthesized from various 4-bromomethyl coumarins 1(a–e). The synthesized compounds were screened for in-vivo analgesic and anti-pyretic activities at a dose of 25 and 100 mg/kg body weight (b.w), respectively. Among them, compounds 5(d), 6(c) and 7(d) exhibited significant analgesic activity comparable with standard drug analgin using Tail-flick model. Compounds 5(a) and 7(a–d) showed significant anti-pyretic activities comparable with standard drug aspirin using yeast-induced pyrexia model. DNA cleavage study by agarose gel electrophoresis method was also studied. Qualitative SAR studies indicate that, compounds with amino group at 2-position of pyrimidine ring enhances analgesic and anti-pyretic activities and compounds with hydroxyl and thio group at 2-position of pyrimidine ring increase DNA cleavage activities.

Graphical abstractA series of new pyrimidine derivatives were synthesized and evaluated for their in-vivo analgesic, anti-pyretic and DNA cleavage studies. Compounds were characterized by spectroscopic studies and elemental analysis.Figure optionsDownload full-size imageDownload as PowerPoint slide