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ID: ALA4385663
Journal: Bioorg Med Chem Lett
Title: Discovery of novel PTHR1 antagonists: Design, synthesis, and structure activity relationships.
Authors: Arai Y, Kiyotsuka Y, Shimada K, Oyama K, Izumi M.
Abstract: The discovery and optimization of a novel series of PTHR1 antagonists are described. Starting from known PTHR1 antagonists, we identified more potent 1,4-benzodiazepin-2-one derivatives by means of a scaffold-hopping approach. The representative compound 23 (DS08210767) exhibited nanomolar-level PTHR1 antagonist activity and potential oral bioavailability in a pharmacokinetic study.
CiteXplore: 31383587