Discovery and biological evaluation of novel 4-amino-2-phenylpyrimidine derivatives as potent and orally active GPR119 agonists

Bioorganic and Medicinal Chemistry

Volumn 20, Issue 17, 2012, Pages 5235-5246

  Negoro, Kenji ^a   Yonetoku, Yasuhiro ^a   Misawa Mukai, Hana ^a   Hamaguchi, Wataru ^a   Maruyama, Tatsuya ^a   Yoshida, Shigeru ^a   Takeuchi, Makoto ^a   Ohta, Mitsuaki ^a  

^a ASTELLAS PHARMA INC   (Japan)

Author keywords

G protein coupled receptor 119; Glucose dependent insulin secretion; GPR119 agonist; Type 2 diabetes mellitus

Indexed keywords

2 (3,4 DICHLOROPHENYL) 6 METHYL N [2 (1 OXIDOPYRIDIN 3 YL)ETHYL]PYRIMIDIN 4 AMINE OXALATE; 2 (4 BROMO 2 FLUOROPHENYL) 6 METHYL N [2 (1 OXIDOPYRIDIN 3 YL)ETHYL]PYRIMIDIN 4 AMINE OXALATE; 2 (4 BROMO 2,5 DIFLUOROPHENYL) 6 METHYL N [2 (1 OXIDOPYRIDIN 3 YL)ETHYL]PYRIMIDIN 4 AMINE OXALATE; 2 (4 BROMO 3 FLUOROPHENYL) 6 METHYL N [2 (1 OXIDOPYRIDIN 3 YL)ETHYL]PYRIMIDIN 4 AMINE OXALATE; 2 (4 BROMO 3,5 DIFLUOROPHENYL) 6 METHYL N [2 (1 OXIDOPYRIDIN 3 YL)ETHYL]PYRIMIDIN 4 AMINE OXALATE; 2 (4 CHLORO 2,5 DIFLUOROPHENYL) 6 METHYL N [2 (1 OXIDOPYRIDIN 3 YL)ETHYL]PYRIMIDIN 4 AMINE OXALATE; 2 (4 CHLORO 3 FLUOROPHENYL) 6 METHYL N [2 (1 OXIDOPYRIDIN 3 YL)ETHYL]PYRIMIDIN 4 AMINE; 2 (4 CHLOROPHENYL) 6 METHYL N [2 (1 OXIDOPYRIDIN 3 YL)ETHYL]PYRIMIDIN 4 AMINE OXALATE; 3 [[2 (4 BROMO 3 FLUOROPHENYL) 6 ETHYLPYRIMIDIN 4 YL]AMINO]PROPANE 1,2 DIOL OXALATE; 3 [[2 (4 BROMO 3 FLUOROPHENYL) 6 METHYLPYRIMIDIN 4 YL]AMINO]PROPANE 1,2 DIOL OXALATE; 3 [[2 (4 CHLORO 2,5 DIFLUOROPHENYL) 6 ETHYLPYRIMIDIN 4 YL]AMINO]PROPANE 1,2 DIOL OXALATE; 3 [[2 (4 CHLORO 3 FLUOROPHENYL) 6 ETHYLPYRIMIDIN 4 YL]AMINO]PROPANE 1,2 DIOL OXALATE; 4 [2 [[2 (4 BROMO 2,5 DIFLUOROPHENYL) 6 METHYLPYRIMIDIN 4 YL]AMINO]ETHYL]PYRIDIN 2(1H) ONE; 4 [2 [[2 (4 BROMO 4 FLUOROPHENYL) 6 METHYLPYRIMIDIN 4 YL]AMINO]ETHYL]PYRIDIN 2(1H) ONE; 4 [2 [[2 (4 CHLORO 2,5 DIFLUOROPHENYL) 6 ETHYLPYRIMIDIN 4 YL]AMINO]ETHYL]PYRIDIN 2(1H) ONE; 4 [2 [[2 (4 CHLORO 2,5 DIFLUOROPHENYL) 6 METHYLPYRIMIDIN 4 YL]AMINO]ETHYL]PYRIDIN 2(1H) ONE; 4 AMINO 2 PHENYLPYRIMIDINE DERIVATIVE; 6 METHYL N [2 (1 OXIDOPYRIDIN 3 YL)ETHYL] 2 PHENYLPYRIMIDIN 4 AMINE OXALATE; ANTIDIABETIC AGENT; G PROTEIN COUPLED RECEPTOR; G PROTEIN COUPLED RECEPTOR 119; GLUCOSE; PIOGLITAZONE; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANTIDIABETIC ACTIVITY; ARTICLE; CONTROLLED STUDY; DIABETES MELLITUS; DRUG BIOAVAILABILITY; DRUG HALF LIFE; DRUG MECHANISM; DRUG POTENCY; DRUG SCREENING; DRUG STRUCTURE; GLUCOSE BLOOD LEVEL; HUMAN; HUMAN CELL; IC 50; IN VITRO STUDY; IN VIVO STUDY; MALE; MOUSE; NON INSULIN DEPENDENT DIABETES MELLITUS; NONHUMAN; ORAL GLUCOSE TOLERANCE TEST; STRUCTURE ACTIVITY RELATION; TIME TO MAXIMUM PLASMA CONCENTRATION;

ADMINISTRATION, ORAL; ANIMALS; CYTOCHROME P-450 CYP1A2; DIABETES MELLITUS, EXPERIMENTAL; DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG DISCOVERY; GLUCOSE TOLERANCE TEST; HAPLORHINI; HEK293 CELLS; HUMANS; HYPOGLYCEMIC AGENTS; MALE; MICE; MICE, INBRED ICR; MOLECULAR STRUCTURE; PYRIMIDINES; RECEPTORS, G-PROTEIN-COUPLED; STRUCTURE-ACTIVITY RELATIONSHIP;

MUS;

EID: 84864995481     PISSN: 09680896     EISSN: 14643391     Source Type: Journal    
DOI: 10.1016/j.bmc.2012.06.049     Document Type: Article

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