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. 2016 Jun 1;26(11):2670-5.
doi: 10.1016/j.bmcl.2016.04.009. Epub 2016 Apr 9.

Optimization of amide-based EP3 receptor antagonists

Esther C Y Lee  1 , Kentaro Futatsugi  2 , Joel T Arcari  3 , Kevin Bahnck  3 , Steven B Coffey  3 , David R Derksen  4 , Amit S Kalgutkar  5 , Paula M Loria  4 , Raman Sharma  4
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Optimization of amide-based EP3 receptor antagonists

Esther C Y Lee et al. Bioorg Med Chem Lett. .

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).

Keywords: EP3 receptor; GPCR; Indazole; LipE; Metabolites; P-gp; PGE2.

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