Identification of (R)-6-(1-(4-cyano-3-methylphenyl)-5-cyclopentyl-4,5-dihydro-1H-pyrazol-3-yl)-2-methoxynicotinic acid, a highly potent and selective nonsteroidal mineralocorticoid receptor antagonist.

Casimiro-Garcia, Agustin; Piotrowski, David W; Ambler, Catherine; Arhancet, Graciela B; Banker, Mary Ellen; Banks, Tereece; Boustany-Kari, Carine M; Cai, Cuiman; Chen, Xiangyang; Eudy, Rena; Hepworth, David; Hulford, Catherine A; Jennings, Sandra M; Loria, Paula M; Meyers, Marvin J; Petersen, Donna N; Raheja, Neil K; Sammons, Matthew; She, Li; Song, Kun; Vrieze, Derek; Wei, Liuqing

Casimiro-Garcia, Agustin; Piotrowski, David W; Ambler, Catherine; Arhancet, Graciela B; Banker, Mary Ellen; Banks, Tereece; Boustany-Kari, Carine M; Cai, Cuiman; Chen, Xiangyang; Eudy, Rena; Hepworth, David; Hulford, Catherine A; Jennings, Sandra M; Loria, Paula M; Meyers, Marvin J; Petersen, Donna N; Raheja, Neil K; Sammons, Matthew; She, Li; Song, Kun; Vrieze, Derek; Wei, Liuqing.

Affiliation

Casimiro-Garcia A; Pfizer Worldwide Research and Development , 200 CambridgePark Drive, Cambridge, Massachusetts 02140, United States.

J Med Chem ; 57(10): 4273-88, 2014 May 22.

Article in En | MEDLINE | ID: mdl-24738581

Subject(s)

Mineralocorticoid Receptor Antagonists/chemical synthesis; Nicotinic Acids/chemical synthesis; Pyrazoles/chemical synthesis; Animals; Drug Discovery; Male; Mineralocorticoid Receptor Antagonists/pharmacology; Molecular Docking Simulation; Nicotinic Acids/pharmacology; Potassium/urine; Pyrazoles/pharmacology; Rats; Rats, Sprague-Dawley; Receptors, Mineralocorticoid/chemistry; Sodium/urine; Structure-Activity Relationship

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Full text: 1 Database: MEDLINE Main subject: Pyrazoles / Mineralocorticoid Receptor Antagonists / Nicotinic Acids Type of study: Diagnostic_studies Limits: Animals Language: En Year: 2014 Type: Article

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