Synthesis and structure-activity relationship of novel RXR antagonists: Orally active anti-diabetic and anti-obesity agents

Bioorganic and Medicinal Chemistry Letters

Volumn 17, Issue 17, 2007, Pages 4804-4807

  Sakaki, Junichi ^a   Kishida, Masashi ^a   Konishi, Kazuhide ^a   Gunji, Hiroki ^a   Toyao, Atsushi ^a   Matsumoto, Yuki ^a   Kanazawa, Takanori ^a   Uchiyama, Hidefumi ^a   Fukaya, Hiroaki ^a   Mitani, Hironobu ^a   Arai, Yoshie ^a   Kimura, Masaaki ^a  

^a NOVARTIS PHARMA AG   (Switzerland)

Author keywords

Antagonist; Anti diabetic; Anti obesity; RXR

Indexed keywords

ANTIDIABETIC AGENT; ANTIOBESITY AGENT; BENZOIC ACID DERIVATIVE; DIAZEPINYLBENZOIC ACID; NITRILE; RECEPTOR BLOCKING AGENT; RETINOID X RECEPTOR; SULFIDE; SULFONE; UNCLASSIFIED DRUG;

ARTICLE; BROMINATION; DRUG ACTIVITY; DRUG RECEPTOR BINDING; DRUG STRUCTURE; DRUG SYNTHESIS; EXPERIMENTAL MODEL; FOOD INTAKE; GLUCOSE BLOOD LEVEL; INSULIN BLOOD LEVEL; NONHUMAN; RECEPTOR BLOCKING; STRUCTURE ACTIVITY RELATION; SUBSTITUTION REACTION; WEIGHT GAIN;

ANIMALS; ANTI-OBESITY AGENTS; BODY WEIGHT; DIETARY FATS; DRUG DESIGN; HYPOGLYCEMIC AGENTS; INHIBITORY CONCENTRATION 50; MALE; MICE; MICE, TRANSGENIC; MODELS, CHEMICAL; RETINOID X RECEPTOR ALPHA; STRUCTURE-ACTIVITY RELATIONSHIP; TRANS-ACTIVATION (GENETICS);

MUS;

EID: 34547531502     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2007.06.080     Document Type: Article

References (11)

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9. See Ref. 6 and references cited therein.
10. 6) δ: 0.99 (3H, s), 1.07 (3H, t), 1.09 (3H, s), 1.19 (3H, t), 1.22 (3H, s), 1.51-1.58 (4H, m), 3.56-3.66 (1H, m), 3.74-3.82 (1H, m), 6.92 (1H, s), 7.02 (1H, s), 7.17 (1H, d), 7.45 (1H, dd), 7.59-7.65 (3H, m), 7.92 (1H, dd), 13.46 (1H, br).
11. For experimental details, see: Sakaki, J; Konishi, K; Kishida, M; Kimura, M; Uchiyiama, H; Mitani, H; WO2004/089916.