Diabetic cardiomyopathy (DCM) is a clinical condition characterized by ventricular dysfunction which develops in diabetic patients in the absence of a coronary disease. The link between the cardiovascular disease and diabetic complications is unveiled by many experimental studies. Activation of PKC-β II, which is a member of protein kinase C (PKC) family, plays a key role in diabetes-induced cardiovascular complications. We have designed Type III peptidomimetics derived from β-secretase peptide crystal structure, which inhibit the binding of receptor for activated C kinases to the C2 domain of PKC-β II. The newly designed peptidomimetics showed good interactions with the active site of PKC-β II in the molecular docking studies. This study may contribute to the development of molecules, which may be useful in the treatment of DCM complications.