Discovery of novel arylpyrazole series as potent and selective opioid receptor-like 1 (ORL1) antagonists

Bioorganic and Medicinal Chemistry Letters

Volumn 19, Issue 13, 2009, Pages 3627-3631

  Kobayashi, Kensuke ^a   Uchiyama, Minaho ^a   Ito, Hirokatsu ^a   Takahashi, Hirobumi ^a   Yoshizumi, Takashi ^a   Sakoh, Hiroki ^a   Nagatomi, Yasushi ^a   Asai, Masanori ^a   Miyazoe, Hiroshi ^a   Tsujita, Tomohiro ^a   Hirayama, Mioko ^a   Ozaki, Satoshi ^a   Tani, Takeshi ^a   Ishii, Yasuyuki ^a   Ohta, Hisashi ^a   Okamoto, Osamu ^a  

^a BANYU PHARMACEUTICAL CO LTD   (Japan)

Author keywords

Arylpyrazole; hERG channel; Nociceptin orphanin FQ; ORL1 antagonist

Indexed keywords

N [[1 (3 CHLOROPYRIDIN 2 YL) 5 (5 FLUORO 6 METHYLPYRIDIN 3 YL) 4 METHYL 1H PYRAZOL 3 YL]METHYL] 3 FLUOROCYCLOPENTANAMINE; OPIOID RECEPTOR LIKE 1 ANTAGONIST; POTASSIUM CHANNEL HERG; PYRAZOLE DERIVATIVE; RECEPTOR BLOCKING AGENT; UNCLASSIFIED DRUG;

ANIMAL CELL; ARTICLE; DRUG POTENCY; DRUG RECEPTOR BINDING; DRUG SELECTIVITY; DRUG STRUCTURE; DRUG SYNTHESIS; EMBRYO; HUMAN; HUMAN CELL; NONHUMAN; REACTION ANALYSIS; STRUCTURE ACTIVITY RELATION; STRUCTURE ANALYSIS;

CYCLOPENTANES; DRUG DISCOVERY; ETHER-A-GO-GO POTASSIUM CHANNELS; HUMANS; PYRAZOLES; RECEPTORS, OPIOID; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 66349099281     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2009.04.116     Document Type: Article

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30. 3) δ (ppm) 1.62-2.32 (9H, m), 2.49 (3H, d, J = 2.9 Hz), 3.31 (1H, quinted, J = 6.3 Hz), 3.93 (2H, s), 5.03-5.22 (1H, m), 7.18 (1H, dd, J = 1.5, 9.8 Hz), 7.31 (1H, dd, J = 4.9, 7.8 Hz), 7.78 (1H, dd, J = 1.5, 7.8 Hz), 8.11 (1H, t, J = 1.5 Hz), 8.43 (1H, dd, J = 1.5, 4.9 Hz).