ANTI-INFLAMMATORY ACTIVITY OF SOME NEW DIHYDROPYRIMIDINES DERIVATIVESAbstract
A series of 6- methyl- 2 – oxo N- (4- oxo- 2- substituted phenyl- 1, 3- thiazolidin- 3- yl)- 4- substituted phenyl- 1, 2, 3, 4- tetrahydropyrimidine- 5- carboxamide have been synthesized and evaluated for their anti-inflammatory activity by carrageenan induced rat paw edema method. The reaction was carried out simply by heating a mixture of three components dissolved in ethanol with a catalytic amount of hydrochloric acid at reflux temperature. The product of this novel one pot, tree-component synthesis that precipitated on cooling of the reaction mixture was identified correctly by Biginelli as 3, 4- dihydropyrimidine- 2 (1H) – one. The synthetic potential of this new heterocyclic synthesis remained unexplored for quite some time. In the 1970s and 1980s interest slowly increased, and the scope of the original cyclocondensation reaction was gradually extended by variation of all three building blocks, allowing access to a large number of multi functionalized dihydropyrimidines. The resulting dihydropyrimidinones and their sulphur analogs posses antibacterial, antiviral, antitumor, anti-inflammatory, antihypertensive as well as calcium channel blocker properties.
Manish Kumar Mishra *, A K Gupta and S Negi
S. G. R. R. I. T. S., Patel Nagar, Dehradun (Uttarakhand), India
18 March, 2010
29 June, 2010
09 July, 2010
01 August, 2010