Abstract: In the present specification we describe a new class of compounds, designed to modulate the ability of blood vessels to synthesize NO from L-arginine. In particular we have identified novel compounds which enhance the entry of L-arginine into cells. These compounds improve endothelial function, and thereby have the potential to retard the progression of vascular disease in conditions such as hypertension, heart failure and diabetes. This new class of drugs may also have other potentially, relevant pharmacological actions, including anti-hypertensive and anti-anginal actions.