Design, synthesis and biological evaluation of a novel class of potent TGR5 agonists based on a 4-phenyl pyridine scaffold

European Journal of Medicinal Chemistry

Volumn 69, Issue , 2013, Pages 55-68

  Zhu, Junjie ^a   Ning, Mengmeng ^a   Guo, Cen ^a   Zhang, Lina ^a   Pan, Guoyu ^a   Leng, Ying ^a   Shen, Jianhua ^a  

^a SHANGHAI INSTITUTE OF MATERIA MEDICA   (China)

Author keywords

4 Phenyl pyridine; Diabetes; GPCR; TGR5

Indexed keywords

(4 PHENYLPYRIDIN 3 YL)METHANAMINE HYDROCHLORIDE; 1 [3,5 BIS(TRIFLUOROMETHYL)PHENYL] N [[4 (2 FLUOROPHENYL)PYRIDIN 3 YL]METHYL]ETHANAMINE; 2 (AZIDOMETHYL) 2' FLUOROBIPHENYL; 2 [3,5 BIS(TRIFLUOROMETHYL)PHENYL] 2 [(4 PHENYLPYRIDIN 3 YL)METHYLAMINO]ACETONITRILE; 2 [3,5 BIS(TRIFLUOROMETHYL)PHENYL] 2 [[4 (2 FLUOROPHENYL)PYRIDIN 3 YL]METHYAMINO]ACETONITRILE; 2 [3,5 BIS(TRIFLUOROMETHYL)PHENYL] 2 [[4 (2,6 FLUOROPHENYL)PYRIDIN 3 YL)METHYLAMINO]ACETONITRILE; 3 (AZIDOMETHYL) 4 (2,6 DIFLUOROPHENYL)PYRIDINE; 3 (AZIDOMETHYL) 4 PHENYL PYRIDINE; [4 (2 FLUOROPHENYL)PYRIDIN 3 YL]METHANAMINE HYDROCHLORIDE; ANTIDIABETIC AGENT; G PROTEIN COUPLED RECEPTOR; N [1 [3,5 BIS(TRIFLUOROMETHYL)PHENYL]ETHYL] N [(4 PHENYLPYRIDIN 3 YL)METHYL]FURAN 2 CARBOXAMIDE; N [1 [3,5 BIS(TRIFLUOROMETHYL)PHENYL]PROPYL] N [(4 PHENYLPYRIDIN 3 YL)METHYL]FURAN 2 CARBOXAMIDE; N [3,5 BIS(TRIFLUOROMETHYL)BENZYL] 1 (4 PHENYLPYRIDIN 3 YL)METHANAMINE; N [3,5 BIS(TRIFLUOROMETHYL)BENZYL] 1 [4 (2 FLUOROPHENYL)PYRIDIN 3 YL]METHANAMINE; N [3,5 BIS(TRIFLUOROMETHYL)BENZYL] 4 CHLORO N [(4 PHENYLPYRIDIN 3 YL)METHYL]BENZAMIDE; N [3,5 BIS(TRIFLUOROMETHYL)BENZYL] N [(4 PHENYLPYRIDIN 3 YL)METHYL]ACETAMIDE; N [3,5 BIS(TRIFLUOROMETHYL)BENZYL] N [(4 PHENYLPYRIDIN 3 YL)METHYL]BENZAMIDE; N [3,5 BIS(TRIFLUOROMETHYL)BENZYL] N [(4 PHENYLPYRIDIN 3 YL)METHYL]CYCLOHEXANECARBOXAMIDE; N [3,5 BIS(TRIFLUOROMETHYL)BENZYL] N [(4 PHENYLPYRIDIN 3 YL)METHYL]FURAN 2 CARBOXAMIDE; N [3,5 BIS(TRIFLUOROMETHYL)BENZYL] N [(4 PHENYLPYRIDIN 3 YL)METHYL]FURAN 3 CARBOXAMIDE; N [3,5 BIS(TRIFLUOROMETHYL)BENZYL] N [(4 PHENYLPYRIDIN 3 YL)METHYL]ISONICOTINAMIDE; N [3,5 BIS(TRIFLUOROMETHYL)BENZYL] N [(4 PHENYLPYRIDIN 3 YL)METHYL]PROPIONAMIDE; N [3,5 BIS(TRIFLUOROMETHYL)BENZYL] N [(4 PHENYLPYRIDIN 3 YL)METHYL]THIOPHENE 2 CARBOXAMIDE; N [3,5 BIS(TRIFLUOROMETHYL)BENZYL] N [(4 PHENYLPYRIDIN 3 YL)METHYL]THIOPHENE 3 CARBOXAMIDE; N [3,5 BIS(TRIFLUOROMETHYL)BENZYL] N [[4 (2 FLUOROPHENYL)PYRIDIN 3 YL]METHYL]FURAN 2 CARBOXAMIDE; N [[4 (2 FLUOROPHENYL)PYRIDIN 3 YL]METHYL] 3,5 BIS(TRIFLUOROMETHYL)BENZAMIDE; N [[4 (2 FLUOROPHENYL)PYRIDIN 3 YL]METHYL] 3,5 BIS(TRIFLUOROMETHYL)BENZENESULFONAMIDE; TAKEDA G PROTEIN COUPLED RECEPTOR; UNCLASSIFIED DRUG; UNINDEXED DRUG;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANTIDIABETIC ACTIVITY; AREA UNDER THE CURVE; ARTICLE; BIOLOGICAL ACTIVITY; CELL STRAIN HEK293; CONTROLLED STUDY; DRUG CLEARANCE; DRUG DESIGN; DRUG HALF LIFE; DRUG POTENCY; DRUG SYNTHESIS; GLUCOSE BLOOD LEVEL; IN VITRO STUDY; IN VIVO STUDY; MOUSE; NONHUMAN; ORAL GLUCOSE TOLERANCE TEST; STRUCTURE ACTIVITY RELATION; SUZUKI REACTION;

4-PHENYL PYRIDINE; DIABETES; GPCR; TGR5;

ANIMALS; DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG DESIGN; GLUCOSE; GLUCOSE TOLERANCE TEST; HUMANS; MALE; MICE; MICE, INBRED ICR; MOLECULAR STRUCTURE; PYRIDINES; RECEPTORS, G-PROTEIN-COUPLED; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 84883231765     PISSN: 02235234     EISSN: 17683254     Source Type: Journal    
DOI: 10.1016/j.ejmech.2013.07.050     Document Type: Article

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