Current Topics in Medicinal Chemistry - Volume 9, Issue 5, 2009

Cardiovascular (CV) disease encompasses coronary heart disease (atherosclerosis), stroke, high blood pressure, heart failure, and several other conditions including arrhythmias, atrial fibrillation, cardiomyopathy and peripheral arterial disease. CV drug discovery over the past few decades has led to some of the most successful drugs on the market. Nevertheless, despite declining death rates in recent years, CV disease re Read More

Epidemiological studies have demonstrated an inverse correlation between plasma concentrations of highdensity lipoprotein cholesterol (HDL-C) and incidence of coronary heart disease (CHD); thus new therapies for raising HDL-C levels have been the focus of significant efforts by the cardiovascular medicine community. Inhibition of cholesteryl ester transfer protein (CETP) is one approach to increasing HDL-C concentr Read More

The discovery of HM74a as a high affinity receptor for nicotinic acid has opened up new areas for investigation. Since its discovery, several new chemical entities have been reported as HM74a agonists. One of them, MK-0354, has been tested in phase II studies, but despite significant decreases in Free Fatty Acid levels with absence of flushing events in clinical studies, it failed to demonstrate effects on LDL-Cholesterol, Read More

The treatment and prevention of atrial fibrillation (AF) remains a significant unmet medical need. Existing therapies that maintain or restore sinus rhythm (rhythm control) have deleterious effects on the ventricle. A major goal for finding new AF therapies is the identification of repolarization mechanisms that are present in the atrium and not in the ventricle. The potassium current IKur has been shown to be selectively involve Read More

Soluble epoxide hydrolase (sEH) is a cross-functional target, with the potential for therapeutic utility in the areas of hypertension, inflammation, and organ-protection [1]. Promising target validation has emerged around soluble epoxide hydrolase in recent years which suggests that small molecule inhibitors may have utility in cardio protection, glucose regulation, hypertension, inflammation, and organ protection. Based o Read More