Discovery of a novel potent Na+/Ca2+ exchanger inhibitor: design, synthesis and structure–activity relationships of 3,4-dihydro-2(1H)-quinazolinone derivatives

Abstract Design, synthesis and structure–activity relationships for 3,4-dihydro-2(1 H )-quinazolinone derivatives with the inhibitory activities of the Na + /Ca 2+ exchanger are discussed. These studies based on lead compound 1a lead to the discovery of a structurally novel and highly potent inhibitor against the Na + /Ca 2+ exchanger 4f ( SM – 15811 ), which directly inhibited the Na + -dependent Ca 2+ influx via the Na + /Ca 2+ exchanger in cardiomyocytes with a high potency.