Discovery of a Potent Free Fatty Acid 1 Receptor Agonist with Low Lipophilicity, Low Polar Surface Area, and Robust in Vivo Efficacy

Journal of Medicinal Chemistry

Volumn 59, Issue 6, 2016, Pages 2841-2846

  Hansen, Steffen V F ^a   Christiansen, Elisabeth ^a   Urban, Christian ^b   Hudson, Brian D ^c   Stocker, Claire J ^d   Due Hansen, Maria E ^a   Wargent, Ed T ^d   Shimpukade, Bharat ^a   Almeida, Reinaldo ^a   Ejsing, Christer S ^a   Cawthorne, Michael A ^d   Kassack, Matthias U ^b   Milligan, Graeme ^c   Ulven, Trond ^a  

^a UNIVERSITY OF SOUTHERN DENMARK   (Denmark)

^b HEINRICH HEINE UNIVERSITY   (Germany)

^c UNIVERSITY OF GLASGOW   (United Kingdom)

^d UNIVERSITY OF BUCKINGHAM   (United Kingdom)

Author keywords

[No Author keywords available]

Indexed keywords

3 [2 FLUORO 4 (3 METHYLPENT 3 EN 1 YN 1 YL)PHENYL]PROPANOIC ACID; ANTIDIABETIC AGENT; G PROTEIN COUPLED RECEPTOR 40; GLUCOSE; INSULIN; UNCLASSIFIED DRUG; 3-(2-FLUORO-4-(3-METHYLPENT-3-EN-1-YN-1-YL)PHENYL)PROPANOIC ACID; G PROTEIN COUPLED RECEPTOR; GLUCOSE BLOOD LEVEL; GPR40 PROTEIN, MOUSE; LIGAND; LIPID; PHENYLPROPIONIC ACID DERIVATIVE;

ANIMAL EXPERIMENT; ARTICLE; BINDING AFFINITY; BINDING SITE; CONTROLLED STUDY; CRYSTAL STRUCTURE; DRUG ABSORPTION; DRUG CLEARANCE; DRUG EFFICACY; DRUG POTENCY; DRUG SOLUBILITY; DRUG SYNTHESIS; GLUCOSE BLOOD LEVEL; GLUCOSE TOLERANCE; HUMAN; IN VIVO STUDY; INSULIN BLOOD LEVEL; INSULIN RESPONSE; LIPOPHILICITY; MAXIMUM PLASMA CONCENTRATION; METABOLIC STABILITY; MOUSE; NONHUMAN; PHYSICAL CHEMISTRY; PLASMA HALF LIFE; RECEPTOR BINDING; SURFACE AREA; AGONISTS; ANIMAL; C57BL MOUSE; CHEMICAL STRUCTURE; CHEMISTRY; DIABETES MELLITUS, TYPE 2; DRUG DEVELOPMENT; GLUCOSE TOLERANCE TEST; METABOLISM; STRUCTURE ACTIVITY RELATION; SYNTHESIS;

ANIMALS; BLOOD GLUCOSE; DIABETES MELLITUS, TYPE 2; DRUG DISCOVERY; GLUCOSE TOLERANCE TEST; HYPOGLYCEMIC AGENTS; LIGANDS; LIPIDS; MICE; MICE, INBRED C57BL; MODELS, MOLECULAR; PHENYLPROPIONATES; RECEPTORS, G-PROTEIN-COUPLED; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 84962189595     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/acs.jmedchem.5b01962     Document Type: Article

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