A simple and efficient microwave-assisted methodology for regioselective alkylation of exocyclic nitrogen of cyclic amidines was developed and novel N-alkylated 3,4-dihydropyrazino [2,1-b] quinazolin-6-ones were prepared. Although none of the molecules tested have any specific anti-quorum sensing (-QS) activity, our result validates the growth tests devised to control the bias of the anti-QS tests. Among the molecules studied, compound 2b exhibits interesting activity against the Gram-negative bacteria Escherichia coli and Shigella sonnei.