Design and evaluation of a novel series of 2,3-oxidosqualene cyclase inhibitors with low systemic exposure, relationship between pharmacokinetic properties and ocular toxicity

Bioorganic and Medicinal Chemistry

Volumn 16, Issue 11, 2008, Pages 6218-6232

  Fouchet, Marie Hélène ^a   Donche, Frédéric ^a   Martin, Christelle ^a   Bouillot, Anne ^a   Junot, Christophe ^a   Boullay, Anne Bénédicte ^a   Potvain, Florent ^a   Magny, Sylvie Demaria ^a   Coste, Hervé ^a   Walker, Max ^b   Issandou, Marc ^a   Dodic, Nérina ^a  

^a GLAXOSMITHKLINE   (France)

^b GLAXOSMITHKLINE   (United States)

Author keywords

2,3 Oxidosqualene:lanosterol cyclase; Hypercholesterolemia; OSC inhibitor; Pharmacophore

Indexed keywords

1 (4 CHLOROPHENYLCARBONYL) 4 [4 (IMIDAZOL 1 YL)PHENYLMETHYL]PIPERAZINE; 1 (4 CHLOROPHENYLSULFONYL) 4 [4 (4 METHYLPIPERAZIN 1 YL)PHENYLMETHYL]PIPERAZINE; 3BETA (2 DIETHYLAMINOETHOXY)ANDROST 5 EN 17 ONE; BIBB 515; ENZYME INHIBITOR; HYDROXYMETHYLGLUTARYL COENZYME A REDUCTASE INHIBITOR; LANOSTEROL SYNTHASE; LANOSTEROL SYNTHASE INHIBITOR; RO48 8071; ZD 9720;

ANIMAL EXPERIMENT; ANIMAL TISSUE; ARTICLE; CATARACT; CHOLESTEROL SYNTHESIS; CONTROLLED STUDY; DOSE RESPONSE; DRUG BLOOD LEVEL; DRUG DESIGN; DRUG LIVER LEVEL; EYE TOXICITY; FEMALE; HUMAN; HUMAN CELL; MALE; NONHUMAN; PHARMACOPHORE; RAT; SINGLE DRUG DOSE;

ANIMALS; ANTICHOLESTEREMIC AGENTS; CATARACT; CELL LINE, TUMOR; DYSLIPIDEMIAS; ENZYME INHIBITORS; EYE; FEMALE; HUMANS; INTRAMOLECULAR TRANSFERASES; LIVER; MALE; OXAZOLES; PIPERAZINES; PIPERIDINES; RATS; RATS, SPRAGUE-DAWLEY;

RATTUS;

EID: 44449115634     PISSN: 09680896     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmc.2008.04.034     Document Type: Article

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