Discovery of AAT-008, a novel, potent, and selective prostaglandin EP4 receptor antagonist.
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Okumura Y, Yamagishi T, Nukui S, Nakao K
Discovery of AAT-008, a novel, potent, and selective prostaglandin EP4 receptor antagonist.
Bioorg Med Chem Lett. 2017 Mar 1;27(5):1186-1192. doi: 10.1016/j.bmcl.2017.01.067. Epub 2017 Jan 25.
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- 28169162 [ View in PubMed]
- Abstract
Starting from acylsufonamide HTS hit 2, a novel series of para-N-acylaminomethylbenzoic acids was identified and developed as selective prostaglandin EP4 receptor antagonists. Structural modifications on lead compound 4a were explored with the aim of improving potency, physicochemical properties, and animal PK predictive of QD (once a day) dosing regimen in human. These efforts led to the discovery of the clinical candidate AAT-008 (4j), which exhibited significantly improved pharmacological profiles over grapiprant (1).
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