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Abstract
Background: Acyl hydroxypyrazoles were discovered and claimed by Merck as novel agonists for the high-affinity nicotinic acid receptor, G-protein coupled receptor 109A (GPR109A). The fused bicyclic core contains a hydroxypyrazole that mimics the anthranilide moiety described in their earlier patents and patent publications. Objective: This article evaluates new GPR109A receptor agonists disclosed by Merck in the recent patent WO2008051403. Conclusion: The aim of this invention was to provide potential therapy to reduce free fatty acids (FFA), low-density lipoprotein cholesterol (LDL-C), total cholesterol, and serum triglycerides (TG), and to raise high-density lipoprotein cholesterol (HDL-C). Thus, these agonists could – potentially – be used to treat dyslipidemia, atherosclerosis, and metabolic syndromes such as diabetes.