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

Article abstract of DOI:10.1016/S0960-894X(03)00744-3

Design, synthesis and structure-activity relationships for 3,4-dihydro-2(1H)-quinazolinone derivatives with the inhibitory activities of the Na⁺/Ca²⁺ 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⁺/Ca²⁺ exchanger 4f (SM-15811), which directly inhibited the Na⁺-dependent Ca ²⁺ influx via the Na⁺/Ca²⁺ exchanger in cardiomyocytes with a high potency.