The synthesis of potent antibacterial agents, free from side effects and resistant to bacterial enzymes, is the main objective for drug designers. Also, the multi-target drugs have important role in advanced drug synthesis. The azo-malonate compounds II a &b were prepared from diazo coupling reaction of aniline derivatives with the acidic methylene group of diethyl malonate. The new azo-malonate derivatives IIa-c were reacted with urea or thiourea in presence of sodium ethoxide, afforded the target new azo-pyrimidine compounds IIIa&b and IV a &b. The structure of the new compounds was elucidated by using NMR, IR, mass spectroscopy and elemental analysis. The MIC of new azo-compounds IIIa&b and IVa&b was evaluated for their antibacterial activity. Two new synthesized compounds showed weak (IIIb) to strong (IVb) antibacterial activity. The MOE docking program was used for prediction of the compound IVb action mechanism.
Key words: Antibacterial; Pyrimidine; Diethyl Malonate; Pyrimidinone
|