Discovery of 2-[4-{{2-(2S,5R)-2-cyano-5-ethynyl-1-pyrrolidinyl]-2-oxoethyl] amino-4-methyl-1-piperidinyl]-4-pyridinecarboxylic acid (ABT-279): A very potent, selective, effective, and well-tolerated inhibitor of dipeptidyl peptidase-IV, useful for the treatment of diabetes

Journal of Medicinal Chemistry

Volumn 49, Issue 21, 2006, Pages 6416-6420

  Madar, David J ^a   Kopecka, Hana ^a   Pireh, Daisy ^a   Yong, Hong ^a   Pei, Zhonghua ^a   Li, Xiaofeng ^a   Wiedeman, Paul E ^a   Djuric, Stevan W ^a   Von Geldern, Thomas W ^a   Fickes, Michael G ^a   Bhagavatula, Lakshmi ^a   McDermott, Todd ^a   Wittenberger, Steven ^a   Richards, Steven J ^a   Longenecker, Kenton L ^a   Stewart, Kent D ^a   Lubben, Thomas H ^a   Ballaron, Stephen J ^a   Stashko, Michael A ^a   Long, Michelle A ^a   Wells, Heidi ^a   Zinker, Bradley A ^a   Mika, Amanda K ^a   Beno, David W A ^a   Kempf Grote, Anita J ^a   Polakowski, James ^a   Segreti, Jason ^a   Reinhart, Glenn A ^a   Fryer, Ryan M ^a   Sham, Hing L ^a   Trevillyan, James M ^a   more..

^a ABBOTT LABORATORIES   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

5 ETHYNYL 1 [N [4 METHYL 1 (4 CARBOXYPYRIDIN 2 YL)PIPERIDIN 4 YL]GLYCYL]PYRROLIDINE 2 CARBONITRILE; ABT 279; ANTIDIABETIC AGENT; DIPEPTIDYL PEPTIDASE 7; DIPEPTIDYL PEPTIDASE 8; DIPEPTIDYL PEPTIDASE 9; DIPEPTIDYL PEPTIDASE IV; DIPEPTIDYL PEPTIDASE IV INHIBITOR; NVP 728; PIPERIDINE DERIVATIVE; PYRIDINE DERIVATIVE; PYRROLIDINE DERIVATIVE; SAXAGLIPTIN; UNCLASSIFIED DRUG; VILDAGLIPTIN;

ANIMAL EXPERIMENT; ANIMAL MODEL; ARTICLE; CONTROLLED STUDY; DOG; DRUG ACTIVITY; DRUG EFFICACY; DRUG INDICATION; DRUG POTENCY; DRUG SAFETY; DRUG SELECTIVITY; DRUG STRUCTURE; DRUG SYNTHESIS; DRUG TOLERABILITY; GLUCOSE TOLERANCE; HUMAN; HUMAN CELL; MONKEY; NON INSULIN DEPENDENT DIABETES MELLITUS; NONHUMAN; RAT; STRUCTURE ACTIVITY RELATION;

ADENOSINE DEAMINASE; ADENOSINE DEAMINASE INHIBITORS; ADMINISTRATION, ORAL; ANIMALS; ANTIGENS, CD26; BINDING SITES; CACO-2 CELLS; CRYSTALLOGRAPHY, X-RAY; DIABETES MELLITUS, TYPE 2; DIPEPTIDYL PEPTIDASE 4; DIPEPTIDYL-PEPTIDASE IV INHIBITORS; DOGS; FEMALE; GLUCOSE INTOLERANCE; GLYCOPROTEINS; HUMANS; HYPOGLYCEMIC AGENTS; MACACA FASCICULARIS; MODELS, MOLECULAR; MOLECULAR STRUCTURE; PYRIDINES; PYRROLIDINES; RATS; RATS, SPRAGUE-DAWLEY; RATS, ZUCKER; STEREOISOMERISM; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 33750116634     PISSN: 00222623     EISSN: None     Source Type: Journal    
DOI: 10.1021/jm060777o     Document Type: Article

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31. DPP9 = 1.76 μM.
32. i for rat DPP-IV is 1.0 nM.