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ID: ALA3797188

Journal: Bioorg Med Chem Lett

Title: Piperidine derivatives as nonprostanoid IP receptor agonists 2.

Authors: Hayashi R, Ito H, Ishigaki T, Morita Y, Miyamoto M, Isogaya M.

Abstract: We searched for a strong and selective nonprostanoid IP agonist bearing piperidine and benzanilide moieties. Through optimization of substituents on the benzanilide moiety, the crucial part of the agonist, 43 (2-((1-(2-(N-(4-tolyl)benzo[d][1,3]dioxole-5-carboxamido)ethyl)piperidin-4-yl)oxy)acetic acid monohydrate monohydrochloride) was discovered and exhibited strong platelet aggregation inhibition (IC50=21nM) and 100-fold selectivity for IP receptor over other PG receptors. The systemic exposure level and bioavailability after oral administration of 43 were also good in dog.

CiteXplore: 27133594

DOI: 10.1016/j.bmcl.2016.04.043