Bioorganic and Medicinal Chemistry Letters
Bioorganic and Medicinal Chemistry Letters
5 years ago

Discovery and SAR of a novel series of Natriuretic Peptide Receptor–A (NPR–A) agonists

Discovery and SAR of a novel series of Natriuretic Peptide Receptor–A (NPR–A) agonists
Novel thienopyrimidine compounds 2 and 3 were discovered from high-throughput screening as Natriuretic Peptide Receptor A (NPR-A) agonists. Scaffold hopping of a thienopyrimidine ring to a quinazoline ring, introduction of the basic functional group and optimization of the substituent on the 6-position of the benzene ring of quinazoline led to improved agonistic activity. We discovered compound 48, which showed potent agonistic activity for NPR-A with an EC50 value of 0.073 μM, indicating 350-fold potency compared to the hit compound 3.

Publisher URL: www.sciencedirect.com/science

DOI: S0960894X1730923X

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