文摘
Recently identified GPCRs, GPR109a and GPR109b, thehigh and low affinity receptors for niacin, may represent good targetsfor the development of HDL elevating drugs for the treatment ofatherosclerosis. Acifran, an agonist of both receptors, has been testedin human subjects, yet until recently very few analogs had been reported.We describe a series of acifran analogs prepared using newly developedsynthetic pathways and evaluated as agonists for GPR109a andGPR109b, resulting in identification of compounds with improvedactivity at these receptors.