Synthesis of 6-oxopyrimidin-1(6H)-yl benzamide derivatives and evaluation of their antibacterial and cytotoxic activity

<p>A series of novel 2-alkylamino and 2, 4-dialkyl amino 6-oxopyrimidin-1(6H)-yl) benzamide derivatives were prepared in good yields from a base-catalyzed ring opening of oxadiazolo[3,2-a]pyrimidin-5-one and evaluated for their antibacterial and cytotoxicity. Most of the compounds exhibited antibacterial activity. In particular, compounds <b>5b</b> and <b>5k</b> exhibited considerable antibiotic activity against <i>Klebsiella pneumonia</i> and <i>Bacillus cereus</i>. In addition, compounds <b>5g</b> and <b>5i</b> also inhibited the growth of two human tumor cell lines (A549 and H460) at micromolar concentrations.</p>