Discovery of a dihydropyrimidine series of molecules that selectively mimic the biological actions of calcitonin

…, W Hageman, RA Rivero, L Westover, M Yang…

Index: Matthews, Jay M.; Liotta, Fina; Hageman, William; Rivero, Ralph A.; Westover, Lori; Yang, Maria; Xu, Jun; Demarest, Keith Bioorganic and Medicinal Chemistry Letters, 2004 , vol. 14, # 5 p. 1155 - 1159

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Citation Number: 9

Abstract

The use of a multiplex mimetic assay led us to identify 1, 4-dihydropyrimidines with potent and selective calcitonin receptor mimetic activity. Subsequent modification of the dihydropyrimidine scaffold led to a series of molecules that were efficacious in a neonatal mouse calvaria in vitro model. Dihydropyrimidine 5h, in particular, was identified as a calcitonin mimetic (EC50= 6 μM), active in-vivo in the Weanling rat model when ...