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

✍ Scribed by Hirohiko Hasegawa; Masami Muraoka; Kazuki Matsui; Atsuyuki Kojima

Publisher
Elsevier Science
Year
2003
Tongue
English
Weight
211 KB
Volume
13
Category
Article
ISSN
0960-894X

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✦ Synopsis

Design, synthesis and structure-activity relationships for 3,4-dihydro-2(1H)-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.

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