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ID: ALA3797093
Journal: Bioorg Med Chem Lett
Title: Optimization of amide-based EP3 receptor antagonists.
Authors: Lee EC, Futatsugi K, Arcari JT, Bahnck K, Coffey SB, Derksen DR, Kalgutkar AS, Loria PM, Sharma R.
Abstract: Prostaglandin E receptor subtype 3 (EP3) antagonism may treat a variety of symptoms from inflammation to cardiovascular and metabolic diseases. Previously, most EP3 antagonists were large acidic ligands that mimic the substrate, prostaglandin E2 (PGE2). This manuscript describes the optimization of a neutral small molecule amide series with improved lipophilic efficiency (LipE) also known as lipophilic ligand efficiency (LLE) ((a) Nat. Rev. Drug Disc.2007, 6, 881; (b) Annu. Rep. Med. Chem.2010, 45, 380).
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