Research Article
Karthikeyan Elumalai, Mohamed
Abstract
We report a library consisting of some novel Biginelli dihydropyrimidines of biological interest as well as their Synthesis of 1,4-dihydropyrimidines by adopting Biginelli synthetic protocol involving one pot multicomponent reaction was performed by following steps as outlined in Scheme (Kappe and Stadler, 2004). In the first step, ethyl acetoacetate 1 and 4-fluro aniline reacted under neat conditions resulting in the formation of N-(4-fluorophenyl)-3- oxobutanamide with the yield of 61%. The N-(4-fluorophenyl)-3-oxobutanamide was further taken for the Biginelli condensation reaction by reacting it with urea or thiourea and aryl or heteroaryl aldehyde in the presence of catalytic amount of p-toluenesulfonic acid (PTSA). synthesis and analysis by TLC, M.P,NMR,IR and Mass spectra. The important steps in the synthetic part were found to be biginelli multicomponent reactions. The synthesized compounds were screened for their in vitro antibacterial activity against two gram-positive bacteria: Staphylococcus aureus and Bacillus subtilis. The title compounds did not exhibit significant antibacterial activity. Furthermore, compounds were subjected to in vitro cytotoxicity against Vero cells. Compounds exhibited weak, moderate, or high cytotoxicity. Compounds 1b, 1c, 1d, 1e, 1f, 1h, 1i, 1n, and 1o exhibited potential cytotoxicity