| Literature DB >> 27107947 |
Esther C Y Lee1, Kentaro Futatsugi2, Joel T Arcari3, Kevin Bahnck3, Steven B Coffey3, David R Derksen4, Amit S Kalgutkar5, Paula M Loria4, Raman Sharma4.
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).Entities:
Keywords: EP3 receptor; GPCR; Indazole; LipE; Metabolites; P-gp; PGE2
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Year: 2016 PMID： 27107947 DOI： 10.1016/j.bmcl.2016.04.009
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823