Design, synthesis and biological evaluation of hetero-aromatic moieties substituted pyrrole-2-carbonitrile derivatives as dipeptidyl peptidase IV inhibitors

European Journal of Medicinal Chemistry

Volumn 75, Issue , 2014, Pages 111-122

  Ji, Xun ^a,b   Su, Mingbo ^b,c   Wang, Jiang ^b   Deng, Guanghui ^b   Deng, Sisi ^b   Li, Zeng ^b   Tang, Chunlan ^b   Li, Jingya ^b   Li, Jia ^b   Zhao, Linxiang ^a   Jiang, Hualiang ^a,b   Liu, Hong ^b  

^a SHENYANG PHARMACEUTICAL UNIVERSITY   (China)

^b SHANGHAI INSTITUTE OF MATERIA MEDICA   (China)

^c EAST CHINA NORMAL UNIVERSITY   (China)

Author keywords

DPP4 inhibitors; Oral bioavailability; Oral glucose tolerance test; Reversible kinetic characterization; Selectivity

Indexed keywords

1 (TERT BUTOXYCARBONYL)PYRROLIDINE 2 CARBOXYLIC ACID; 1 [2 AMINO 3 (2 METHYLTHIAZOL 4 YL)PROPANOYL] 4 FLUOROPYRROLIDINE 2 CARBONITRILE; 1 [2 AMINO 3 (2 PHENYLLTHIAZOL 4 YL)PROPANOYL] 4 FLUOROPYRROLIDINE 2 CARBONITRILE; 1 [2 AMINO 3 (6 BROMOBENZO[D][1,3]DIOXOL 5 YL)PROPANOYL] 4 FLUOROPYRROLIDINE 2 CARBONITRILE; 1 [2 AMINO 3 (BENZO[B]THIOPHEN 3 YL)PROPANOYL] 4 FLUOROPYRROLIDINE 2 CARBONITRILE; 1 [2 AMINO 3 (BENZO[B]THIOPHEN 3 YL)PROPANOYL]PYRROLIDINE 2 CARBONITRILE; 1 [2 AMINO 3 (FURAN 3 YL)PROPANOYL]PYRROLIDINE 2 CARBONITRILE; 1 [2 AMINO 3 (PYRIDIN 2 YL)PROPANOYL]PYRROLIDINE 2 CARBONITRILE; 1 [2 AMINO 3 (THIAZOL 4 YL)PROPANOYL] 4 FLUOROPYRROLIDINE 2 CARBONITRILE; 1 [2 AMINO 3 (THIAZOL 4 YL)PROPANOYL]PYRROLIDINE 2 CARBONITRILE; 1 [2 AMINO 3 (THIOPHEN 2 YL)PROPANOYL] 4 FLUOROPYRROLIDINE 2 CARBONITRILE; 1 [2 AMINO 3 (THIOPHEN 3 YL)PROPANOYL]PYRROLIDINE 2 CARBONITRILE; 1 [2 AMINO 3 [2 (4 CHLOROPHENYL)THIAZOL 4 YL]PROPANOYL] 4 FLUOROPYRROLIDINE 3 CARBONITRILE; 1 [2 AMINO 3 [2 (THIOPHEN 2 YL)THIAZOL 4 YL]PROPANOYL 4 FLUOROPYRROLIDINE 2 CARBONITRILE; 1 [2 AMINO 3 [2 [4 (TRIFLUOROMETHYL)PHENYL]THIAZOL 3 YL]PROPANOYL] 4 FLUOROPYRROLIDINE 2 CARBONITRILE; ANTIDIABETIC AGENT; CYANIDE; DIPEPTIDYL PEPTIDASE IV INHIBITOR; PYRROLIDINE 2 CARBONITRILE 4 METHYLBENZENE 1 SULFONIC ACID; PYRROLIDINE DERIVATIVE; SITAGLIPTIN; TERT BUTYL 2 CARBAMOYLPYRROLIDINE 1 CARBOXYLATE; TERT BUTYL 2 CYANOPYRROLIDINE 1 CARBOXYLATE; TERT BUTYL N [1 [2 CYANOPYRROLIDIN 1 YL] 1 OXO 3 (BENZO[B]THIOPHEN 3 YL)PROPAN 2 YL]CARBAMATE; TERT BUTYL N [1 [2 CYANOPYRROLIDIN 1 YL] 1 OXO 3 (PYRIDIN 2 YL)PROPAN 2 YL]CARBAMATE; TERT BUTYL N [1 [2 CYANOPYRROLIDIN 1 YL] 1 OXO 3 (THIAZOL 4 YL)PROPAN 2 YL]CARBAMATE; TERT BUTYL N [1 [2 CYANOPYRROLIDIN 1 YL] 1 OXO 3 (THIOPHEN 3 YL)PROPAN 2 YL]CARBAMATE; TERT BUTYL N [1 [2 CYANOPYRROLIDIN 1 YL] 3 (FURAN 3 YL) 1 OXOPROPAN 2 YL]CARBAMATE; UNCLASSIFIED DRUG; UNINDEXED DRUG; VILDAGLIPTIN;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANTIDIABETIC ACTIVITY; AREA UNDER THE CURVE; ARTICLE; CONTROLLED STUDY; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG CLEARANCE; DRUG DESIGN; DRUG HALF LIFE; DRUG SYNTHESIS; ENZYME ASSAY; ENZYME INHIBITION; GLUCOSE BLOOD LEVEL; IC 50; IN VITRO STUDY; IN VIVO STUDY; LIQUID CHROMATOGRAPHY; MOUSE; MULTIPLE DRUG DOSE; NON INSULIN DEPENDENT DIABETES MELLITUS; NONHUMAN; ORAL GLUCOSE TOLERANCE TEST; SINGLE DRUG DOSE; STRUCTURE ACTIVITY RELATION; TANDEM MASS SPECTROMETRY;

DPP4 INHIBITORS; ORAL BIOAVAILABILITY; ORAL GLUCOSE TOLERANCE TEST; REVERSIBLE KINETIC CHARACTERIZATION; SELECTIVITY;

ANIMALS; CELL LINE; DIABETES MELLITUS, TYPE 2; DIPEPTIDYL PEPTIDASE 4; DIPEPTIDYL-PEPTIDASE IV INHIBITORS; DRUG DESIGN; GLUCOSE TOLERANCE TEST; HUMANS; HYPOGLYCEMIC AGENTS; MICE; MICE, INBRED ICR; MODELS, MOLECULAR; NITRILES; PYRROLES; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 84894213836     PISSN: 02235234     EISSN: 17683254     Source Type: Journal    
DOI: 10.1016/j.ejmech.2014.01.021     Document Type: Article

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