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

作者：Keri Rangappa S; Hosamani Kallappa M^*; Shingalapur Ramya V; Hugar Mallinath H

来源：European Journal of Medicinal Chemistry, 2010, 45(6): 2597-2605.

DOI：10.1016/j.ejmech.2010.02.048

• Pyrimidine
• Coumarin
• Analgesic
• Anti-pyretic
• DNA cleavage

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 till group at 2-position of pyrimidine ring increase DNA cleavage activities.

• 出版日期2010-6