Bioorganic & medicinal chemistry letters, 2013-12, Vol.23 (23), p.6459-6462
- Martinez-Perez, Jose A.
- Iyengar, Smriti
- Shannon, Harlan E.
- Bleakman, David
- Alt, Andrew
- Arnold, Brian M.
- Bell, Michael G.
- Bleisch, Thomas J.
- Castaño, Ana M.
- Del Prado, Miriam
- Dominguez, Esteban
- Escribano, Ana M.
- Filla, Sandra A.
- Ho, Ken H.
- Hudziak, Kevin J.
- Jones, Carrie K.
- Mateo, Ana
- Mathes, Brian M.
- Mattiuz, Edward L.
- Ogden, Ann Marie L.
- Simmons, Rosa Maria A.
- Stack, Douglas R.
- Stratford, Robert E.
- Winter, Mark A.
- Wu, Zhipei
- Ornstein, Paul L.
2013
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- Autor(en) / Beteiligte
- Martinez-Perez, Jose A.
- Iyengar, Smriti
- Shannon, Harlan E.
- Bleakman, David
- Alt, Andrew
- Arnold, Brian M.
- Bell, Michael G.
- Bleisch, Thomas J.
- Castaño, Ana M.
- Del Prado, Miriam
- Dominguez, Esteban
- Escribano, Ana M.
- Filla, Sandra A.
- Ho, Ken H.
- Hudziak, Kevin J.
- Jones, Carrie K.
- Mateo, Ana
- Mathes, Brian M.
- Mattiuz, Edward L.
- Ogden, Ann Marie L.
- Simmons, Rosa Maria A.
- Stack, Douglas R.
- Stratford, Robert E.
- Winter, Mark A.
- Wu, Zhipei
- Ornstein, Paul L.
- Titel
- GluK1 antagonists from 6-(carboxy)phenyl decahydroisoquinoline derivatives. SAR and evaluation of a prodrug strategy for oral efficacy in pain models
- Ist Teil von
- Bioorganic & medicinal chemistry letters, 2013-12, Vol.23 (23), p.6459-6462
- Ort / Verlag
- England: Elsevier Ltd
- Erscheinungsjahr
- 2013
- Quelle
- Elsevier ScienceDirect Journals
- Beschreibungen/Notizen
- The synthesis and structure–activity relationship of decahydroisoquinoline derivatives with various benzoic acid substitutions as GluK1 antagonists are described. Potent and selective antagonists were selected for a tailored prodrug approach in order to facilitate the evaluation of the new compounds in pain models after oral administration. Several diester prodrugs allowed for acceptable amino acid exposure and moderate efficacy in vivo.
- Sprache
- Englisch
- Identifikatoren
- ISSN: 0960-894XeISSN: 1464-3405DOI: 10.1016/j.bmcl.2013.09.046Titel-ID: cdi_proquest_miscellaneous_1500769539
- Format
- –
- Schlagworte
- Administration, Oral, Amino Acid Sequence, Amino acids, Animals, antagonists, benzoic acid, Decahydroisoquinolines, Disease Models, Animal, GluA2, GluK1 antagonists, Haplorhini, Isoquinolines - chemistry, Isoquinolines - pharmacology, Molecular Sequence Data, oral administration, Pain, Pain - drug therapy, Prodrug, Prodrugs - chemistry, Prodrugs - pharmacology, Receptors, Kainic Acid - antagonists & inhibitors, Receptors, Kainic Acid - chemistry, Structure-Activity Relationship, structure-activity relationships