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Bioorganic and Medicinal Chemistry Letters

Volumn 24, Issue 17, 2014, Pages 4271-4275

Discovery of novel pyrimidine and malonamide derivatives as TGR5 agonists

(13) Park, Eun Ju a,b Ahn, Young Gil a Jung, Seung Hyun a Bang, Hyo Jeong a,b Kim, Mira a,b Hong, Dong Jin a,b Kim, Jisook a Suh, Kwee Hyun a Kim, Young Jin b Kim, Doran b Kim, Eun Yeong c Lee, Kiho c Min, Kyung Hoon b

a Hanmi Pharmaceutical Co Ltd (South Korea)

b Chung Ang University (South Korea)

c Korea University (South Korea)

Author keywords

Agonist; Bioisostere; Malonamide; Pyrimidine; TGR5

Indexed keywords

CYCLOPROPYLMALONAMIDE DERIVATIVE; CYTOCHROME P450 1A2; CYTOCHROME P450 2C19; CYTOCHROME P450 2C9; CYTOCHROME P450 2D6; CYTOCHROME P450 3A4; G PROTEIN COUPLED RECEPTOR; PYRIMIDINE DERIVATIVE; TAKEDA G PROTEIN COUPLED RECEPTOR 5; TAKEDA G PROTEIN COUPLED RECEPTOR 5 AGONIST; UNCLASSIFIED DRUG; CYTOCHROME P450; CYTOCHROME P450 INHIBITOR; GPBAR1 PROTEIN, HUMAN; MALONAMIDE; MALONIC ACID DERIVATIVE; PYRIMIDINE;

ANIMAL EXPERIMENT; AREA UNDER THE CURVE; ARTICLE; CONTROLLED STUDY; DRUG BIOAVAILABILITY; DRUG DISTRIBUTION; DRUG HALF LIFE; DRUG HYDROLYSIS; DRUG POTENCY; DRUG STRUCTURE; DRUG SYNTHESIS; ENZYME INHIBITION; HUMAN; HUMAN CELL; IC 50; MALE; MAXIMUM PLASMA CONCENTRATION; MEAN RESIDENCE TIME; MOUSE; NONHUMAN; SUBSTITUTION REACTION; TIME TO MAXIMUM PLASMA CONCENTRATION; AGONISTS; ANIMAL; BIOAVAILABILITY; CHEMICAL STRUCTURE; CHEMISTRY; DOSE RESPONSE; DRUG DEVELOPMENT; DRUG EFFECTS; ENZYMOLOGY; HEK293 CELL LINE; INSTITUTE FOR CANCER RESEARCH MOUSE; LIVER MICROSOME; METABOLISM; STRUCTURE ACTIVITY RELATION;

ANIMALS; BIOLOGICAL AVAILABILITY; CYTOCHROME P-450 ENZYME INHIBITORS; CYTOCHROME P-450 ENZYME SYSTEM; DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG DISCOVERY; HEK293 CELLS; HUMANS; MALONATES; MICE; MICE, INBRED ICR; MICROSOMES, LIVER; MOLECULAR STRUCTURE; PYRIMIDINES; RECEPTORS, G-PROTEIN-COUPLED; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 84906933589 PISSN: 0960894X EISSN: 14643405 Source Type: Journal
DOI: 10.1016/j.bmcl.2014.07.026 Document Type: Article

Times cited : (11)

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