Discovery of C-(1-aryl-cyclohexyl)-methylamines as selective, orally available inhibitors of dipeptidyl peptidase IV

Bioorganic and Medicinal Chemistry Letters

Volumn 24, Issue 3, 2014, Pages 731-736

  Namoto, Kenji ^a   Sirockin, Finton ^a   Ostermann, Nils ^a   Gessier, Francois ^a   Flohr, Stefanie ^a   Sedrani, Richard ^a   Gerhartz, Bernd ^a   Trappe, Jörg ^a   Hassiepen, Ulrich ^a   Duttaroy, Alokesh ^b   Ferreira, Suzie ^b   Sutton, Jon M ^c   Clark, David E ^c   Fenton, Garry ^c   Beswick, Mandy ^c   Baeschlin, Daniel K ^a  

^a NOVARTIS PHARMA AG   (Switzerland)

^b NOVARTIS INSTITUTES FOR BIOMEDICAL RESEARCH   (United States)

^c Argenta Discovery Ltd   (United Kingdom)

Author keywords

Dipeptidyl peptidase IV; Enzyme selectivity; Ex vivo plasma DPP IV inhibition; Pharmacokinetics; Protease inhibition; Structure based drug design

Indexed keywords

C (1 ARYL CYCLOHEXYL) METHYLAMINE; DIPEPTIDYL PEPTIDASE IV INHIBITOR; SITAGLIPTIN; UNCLASSIFIED DRUG; VILDAGLIPTIN;

ANIMAL EXPERIMENT; ARTICLE; CRYSTAL STRUCTURE; DRUG BIOAVAILABILITY; DRUG CLEARANCE; DRUG PENETRATION; DRUG SYNTHESIS; IC 50; NONHUMAN; RAT; STRUCTURE ACTIVITY RELATION;

RATTUS;

DIPEPTIDYL PEPTIDASE IV; ENZYME SELECTIVITY; EX VIVO PLASMA DPP IV INHIBITION; PHARMACOKINETICS; PROTEASE INHIBITION; STRUCTURE-BASED DRUG DESIGN;

ADAMANTANE; ADMINISTRATION, ORAL; ANIMALS; CACO-2 CELLS; CRYSTALLOGRAPHY, X-RAY; CYCLIZATION; DIPEPTIDYL PEPTIDASE 4; DIPEPTIDYL-PEPTIDASE IV INHIBITORS; DRUG DISCOVERY; ENZYME ACTIVATION; HUMANS; INHIBITORY CONCENTRATION 50; METHYLAMINES; MOLECULAR STRUCTURE; NITRILES; PYRAZINES; PYRROLIDINES; RATS; TRIAZOLES;

EID: 84893655057     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2013.12.118     Document Type: Article

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