Facile Diversity-Oriented Synthesis of Novel Dipeptide Mimetic Compounds Containing Bioactive Molecular Skeletons under Microwave Irradiation

The diversity-oriented synthesis of dipeptide mimetic compounds embedded with bioactive molecular skeletons have been successfully established via microwave-assisted reactions between various 4-arylidene-2-phenyloxazol-5(4H)-ones and a broad scope of amines including aliphatic, aromatic, and heteroaromatic ones. This synthetic approach has prominent features of short reaction time, high yields, operational simplicity,as well as widespread applications, leading to a facile and straightforward access to structurally diverse dipeptide analogues with, potential bioactivities, Moreover, the preliminary evaluation on the cytotoxic activity of this type-of dipeptide derivatives has resulted in the finding of five Compounds with stronger cytotoxicity than doxorubicin hydrochloride at the concentration of 10 mu g/mL.