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Optimization of amide-based EP3 receptor antagonists.
Lee, Esther C Y; Futatsugi, Kentaro; Arcari, Joel T; Bahnck, Kevin; Coffey, Steven B; Derksen, David R; Kalgutkar, Amit S; Loria, Paula M; Sharma, Raman.
Afiliación
  • Lee EC; Worldwide Medicinal Chemistry, Pfizer Worldwide Research & Development, Cambridge, MA 02139, United States. Electronic address: esther.lee2@pfizer.com.
  • Futatsugi K; Worldwide Medicinal Chemistry, Pfizer Worldwide Research & Development, Cambridge, MA 02139, United States.
  • Arcari JT; Worldwide Medicinal Chemistry, Pfizer Worldwide Research & Development, Groton, CT 06340, United States.
  • Bahnck K; Worldwide Medicinal Chemistry, Pfizer Worldwide Research & Development, Groton, CT 06340, United States.
  • Coffey SB; Worldwide Medicinal Chemistry, Pfizer Worldwide Research & Development, Groton, CT 06340, United States.
  • Derksen DR; Pharmacokinetics, Dynamics, and Metabolism, Pfizer Worldwide Research & Development, Groton, CT 06340, United States.
  • Kalgutkar AS; Pharmacokinetics, Dynamics and Metabolism, Pfizer Worldwide Research & Development, Cambridge, MA 02139, United States.
  • Loria PM; Pharmacokinetics, Dynamics, and Metabolism, Pfizer Worldwide Research & Development, Groton, CT 06340, United States.
  • Sharma R; Pharmacokinetics, Dynamics, and Metabolism, Pfizer Worldwide Research & Development, Groton, CT 06340, United States.
Bioorg Med Chem Lett ; 26(11): 2670-5, 2016 06 01.
Article en En | MEDLINE | ID: mdl-27107947
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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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Subtipo EP3 de Receptores de Prostaglandina E / Amidas Límite: Humans Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2016 Tipo del documento: Article Pais de publicación: Reino Unido
Texto completo
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Subtipo EP3 de Receptores de Prostaglandina E / Amidas Límite: Humans Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2016 Tipo del documento: Article Pais de publicación: Reino Unido