Discovery and structure-activity relationships of pentanedioic acid diamides as potent inhibitors of 11β-hydroxysteroid dehydrogenase type I

Bioorganic and Medicinal Chemistry Letters

Volumn 19, Issue 10, 2009, Pages 2674-2678

  Roche, Didier ^a   Carniato, Denis ^a   Leriche, Caroline ^a   Lepifre, Franck ^a   Christmann Franck, Serge ^a   Graedler, Ulrich ^b   Charon, Christine ^a   Bozec, Sophie ^a   Doare, Liliane ^a   Schmidlin, Fabien ^a   Lecomte, Marc ^a   Valeur, Eric ^a  

^a Merck KGaA France   (France)

^b Merck Serono GmbH   (Germany)

Author keywords

11 Hydroxysteroid dehydrogenase type I inhibitors; Lead optimisation; Pentanedioic acid diamides; Rational drug design

Indexed keywords

11BETA HYDROXYSTEROID DEHYDROGENASE 1; 11BETA HYDROXYSTEROID DEHYDROGENASE 1 INHIBITOR; 11BETA HYDROXYSTEROID DEHYDROGENASE 2; ADAMANTANE DERIVATIVE; DIAMIDE; GLUTARIC ACID DERIVATIVE; OXIDOREDUCTASE INHIBITOR; UNCLASSIFIED DRUG;

ADIPOCYTE; ANIMAL CELL; ANIMAL EXPERIMENT; ARTICLE; DRUG CLEARANCE; DRUG DISTRIBUTION; DRUG HALF LIFE; DRUG IDENTIFICATION; DRUG POTENCY; DRUG SELECTIVITY; DRUG SOLUBILITY; ENZYME INHIBITION; HIGH THROUGHPUT SCREENING; HUMAN; IC 50; MALE; MOUSE; NONHUMAN; RAT; STRUCTURE ACTIVITY RELATION;

11-BETA-HYDROXYSTEROID DEHYDROGENASE TYPE 1; 11-BETA-HYDROXYSTEROID DEHYDROGENASE TYPE 2; 3T3-L1 CELLS; AMIDES; ANIMALS; DRUG DISCOVERY; ENZYME INHIBITORS; HUMANS; MICE; RATS; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 65349167925     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2009.03.140     Document Type: Article

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