Discovery and Preclinical Characterization of 6-Chloro-5-[4-(1-hydroxycyclobutyl)phenyl]-1H-indole-3-carboxylic Acid (PF-06409577), a Direct Activator of Adenosine Monophosphate-activated Protein Kinase (AMPK), for the Potential Treatment of Diabetic Nephropathy

Journal of Medicinal Chemistry

Volumn 59, Issue 17, 2016, Pages 8068-8081

  Cameron, Kimberly O ^a   Kung, Daniel W ^a   Kalgutkar, Amit S ^a   Kurumbail, Ravi G ^a   Miller, Russell ^a   Salatto, Christopher T ^a   Ward, Jessica ^a   Withka, Jane M ^a   Bhattacharya, Samit K ^a   Boehm, Markus ^a   Borzilleri, Kris A ^a   Brown, Janice A ^a   Calabrese, Matthew ^a   Caspers, Nicole L ^a   Cokorinos, Emily ^a   Conn, Edward L ^a   Dowling, Matthew S ^a   Edmonds, David J ^a   Eng, Heather ^a   Fernando, Dilinie P ^a   Frisbie, Richard ^a   Hepworth, David ^a   Landro, James ^a   Mao, Yuxia ^a   Rajamohan, Francis ^a   Reyes, Allan R ^a   Rose, Colin R ^a   Ryder, Tim ^a   Shavnya, Andre ^a   Smith, Aaron C ^a   Tu, Meihua ^a   Wolford, Angela C ^a   Xiao, Jun ^a   more..

^a PFIZER INC   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

5 (4 METHOXYPHENYL) 1H INDAZOLE 3 CARBOXYLIC ACID; 6 CHLORO 5 (2 HYDROXYBIPHENYL 4 YL) 1H INDOLE 3 CARBOXYLIC ACID; 6 CHLORO 5 (4 METHOXYPHENYL) 1H INDAZOLE 3 CARBOXYLIC ACID; 6 CHLORO 5 (4 METHOXYPHENYL) 1H INDOLE 3 CARBOXYLIC ACID; 6 CHLORO 5 [4 (1 HYDROXYCYCLOBUTYL)PHENYL] 1H INDOLE 3 CARBOXYLIC ACID; 6 CHLORO 5 [4 (HYDROXYMETHYL)PHENYL] 1H INDOLE 3 CARBOXYLIC ACID; ADENYLATE KINASE; CARBOXYLIC ACID DERIVATIVE; ENZYME ACTIVATOR; N (2 HYDROXY 1 PHENYLETHYL) 5 (4 METHOXYPHENYL) 1H INDAZOLE 3 CARBOXAMIDE; RAMIPRIL; UNCLASSIFIED DRUG; HYDROXYMETHYLGLUTARYL COENZYME A REDUCTASE KINASE; INDAZOLE DERIVATIVE; INDOLE DERIVATIVE; PF-6409577;

ANIMAL CELL; ANIMAL EXPERIMENT; ARTICLE; CONTROLLED STUDY; CRYSTAL STRUCTURE; DIABETIC NEPHROPATHY; DOG; DRUG ABSORPTION; DRUG BIOAVAILABILITY; DRUG DISPOSITION; DRUG PENETRATION; DRUG POTENCY; DRUG SOLUBILITY; HAPLORHINI; HUMAN; HUMAN CELL; IN VITRO STUDY; IN VIVO STUDY; NONHUMAN; PHYSICAL CHEMISTRY; PLASMA PROTEIN BINDING; RAT; ADSORPTION; ANIMAL; CHEMISTRY; DIABETIC NEPHROPATHIES; HIGH THROUGHPUT SCREENING; INTRAVENOUS DRUG ADMINISTRATION; MACACA FASCICULARIS; MALE; METABOLISM; MOLECULAR MODEL; ORAL DRUG ADMINISTRATION; PROTEIN CONFORMATION; SYNTHESIS; X RAY CRYSTALLOGRAPHY;

ADMINISTRATION, ORAL; ADSORPTION; AMP-ACTIVATED PROTEIN KINASES; ANIMALS; CRYSTALLOGRAPHY, X-RAY; DIABETIC NEPHROPATHIES; DOGS; ENZYME ACTIVATORS; HIGH-THROUGHPUT SCREENING ASSAYS; HUMANS; INDAZOLES; INDOLES; INJECTIONS, INTRAVENOUS; MACACA FASCICULARIS; MALE; MODELS, MOLECULAR; PROTEIN CONFORMATION; RATS;

EID: 84986538891     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/acs.jmedchem.6b00866     Document Type: Article

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