Aromatic-substituted derivatives of 1,3,2-diazaphospholidin-4-ones 2a-g were readily prepared front 1,3-diaryl glycinamides 1 by the reaction with hexaethylphosphoric triamide. Their chemical transformation was selectively effected with different thionation reagents to afford thionated products at the phosphorus atom to give 3a-g and at the carbonyl group to give 4a. An oxidation reaction at phosphorus to produce 5a was effected with 10% hydrogen peroxide. Preliminary bioassays revealed that some of the title compounds, 2a-g and 3a-g, possess select...