Identification of 4H,6H-[2]benzoxepino[4,5-c][1,2]oxazoles as novel squalene synthase inhibitors

Bioorganic and Medicinal Chemistry Letters

Volumn 21, Issue 12, 2011, Pages 3648-3653

  Griebenow, Nils ^a   Buchmueller, Anja ^a   Kolkhof, Peter ^a   Schamberger, Jens ^a   Bischoff, Hilmar ^a  

^a BAYER PHARMA AG   (Germany)

Author keywords

4H,6H 2 Benzoxepino 4,5 c 1,2 oxazole; Atherosclerosis; SAR; Squalene synthase inhibitor

Indexed keywords

4H,6H [2]BENZOXEPINO[4,5 C][1,2]OXAZOLE DERIVATIVE; LAPAQUISTAT; OXAZOLE DERIVATIVE; SQUALENE SYNTHASE INHIBITOR; UNCLASSIFIED DRUG;

ARTICLE; CROSS COUPLING REACTION; DRUG DESIGN; DRUG POTENCY; DRUG STABILITY; DRUG STRUCTURE; DRUG SYNTHESIS; IC 50; NONHUMAN; PHYSICAL CHEMISTRY; STEREOCHEMISTRY; STRUCTURE ACTIVITY RELATION;

BINDING SITES; CRYSTALLOGRAPHY, X-RAY; DRUG DESIGN; ENZYME ACTIVATION; ENZYME INHIBITORS; FARNESYL-DIPHOSPHATE FARNESYLTRANSFERASE; INHIBITORY CONCENTRATION 50; MOLECULAR STRUCTURE; OXAZOLES; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 79957811546     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2011.04.092     Document Type: Article

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39. +.
40. Intrument: Micromass Quattro LCZ with HPLC Agilent Series 1100; column: Phenomenex Synergi 2 μ Hydro-RP Mercury, 20 x 4 mm; eluent A: 1 l water + 0.5 ml 50% formic acid; eluent B: 1 l acetonirile + 0.5 ml 50% formic acid; gradient: 0.0 min 90% A→2.5 min 30% A→3.0 min 5% A→4.5 min 5% A; flow rate: 0.0 min 1 ml/min→2.5 min/3.0 min/4.5 min 2 ml/min; oven: 50 °C; UV detection: 208-400 nm.