Synthesis and evaluation of novel stearoyl-CoA desaturase 1 inhibitors: 1′-{6-[5-(pyridin-3-ylmethyl)-1,3,4-oxadiazol-2-yl]pyridazin-3-yl}-3, 4-dihydrospiro[chromene-2,4′-piperidine] analogs

European Journal of Medicinal Chemistry

Volumn 45, Issue 11, 2010, Pages 4788-4796

  Uto, Yoshikazu ^a   Ueno, Yuko ^a   Kiyotsuka, Yohei ^a   Miyazawa, Yuriko ^a   Kurata, Hitoshi ^a   Ogata, Tsuneaki ^a   Yamada, Makiko ^a   Deguchi, Tsuneo ^a   Konishi, Masahiro ^a   Takagi, Toshiyuki ^a   Wakimoto, Satoko ^a   Ohsumi, Jun ^a  

^a DAIICHI SANKYO CO   (Japan)

Author keywords

Oxadiazole; SCD1 inhibitor; Spiropiperidine

Indexed keywords

1' [6 [5 (PYRIDIN 3 YLMETHYL) 1,3,4 OXADIAZOL 2 YL]PYRIDAZIN 3 YL] 5 (TRIFLUOROMETHYL) 3,4 DIHYDROSPIRO[CHROMENE 2,40 PIPERIDINE]; 10 [6 [5 (PYRIDIN 2 YLMETHYL) 1,3,4 OXADIAZOL 2 YL]PYRIDAZIN 3 YL] 3,4 DIHYDROSPIRO[CHROMENE 2,40 PIPERIDINE]; 10 [6 [5 (PYRIDIN 3 YLMETHYL) 1,3,4 OXADIAZOL 2 YL]PYRIDAZIN 3 YL] 3,4 DIHYDROSPIRO[CHROMENE 2,40 PIPERIDINE]; 10 [6 [5 (PYRIDIN 4 YLMETHYL) 1,3,4 OXADIAZOL 2 YL]PYRIDAZIN 3 YL] 3,4 DIHYDROSPIRO[CHROMENE 2,40 PIPERIDINE]; 5 CHLORO 1' [6 [5 (PYRIDIN 3 YLMETHYL) 1,3,4 OXADIAZOL 2 YL]PYRIDAZIN 3 YL] 3,4 DIHYDROSPIRO[CHROMENE 2,40 PIPERIDINE]; 5 FLUORO 10 [6 [5 (PYRIDIN 3 YLMETHYL) 1,3,4 OXADIAZOL 2 YL]PYRIDAZIN 3 YL] 3,4 DIHYDROSPIRO[CHROMENE 2,40 PIPERIDINE]; 5 METHYL 10 [6 [5 (PYRIDIN 3 YLMETHYL) 1,3,4 OXADIAZOL 2 YL]PYRIDAZIN 3 YL] 3,4 DIHYDROSPIRO[CHROMENE 2,40 PIPERIDINE]; 5,8 DIFLUORO 10 [6 [5 (PYRIDIN 3 YLMETHYL) 1,3,4 OXADIAZOL 2 YL]PYRIDAZIN 3 YL] 3,4 DIHYDROSPIRO[CHROMENE 2,40 PIPERIDINE]; 6 (3,4 DIHYDRO 10H SPIRO[CHROMENE 2,40 PIPERIDIN] 10 YL)N(2 PYRIDIN 3 YLETHYL)PYRIDAZINE 3 CARBOXAMIDE; ENZYME INHIBITOR; STEAROYL COENZYME A DESATURASE 1 INHIBITOR; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; AREA UNDER THE CURVE; ARTICLE; C57BL 6 MOUSE; CARBOHYDRATE DIET; CHEMICAL MODIFICATION; DOSE RESPONSE; DRUG BIOAVAILABILITY; DRUG CLEARANCE; DRUG HALF LIFE; DRUG MEGADOSE; DRUG POTENCY; DRUG SOLUBILITY; DRUG STRUCTURE; DRUG SYNTHESIS; ENZYME INHIBITION; EVALUATION; HUMAN; HUMAN CELL; IC 50; MAXIMUM PLASMA CONCENTRATION; MOUSE; NONHUMAN; TIME TO MAXIMUM PLASMA CONCENTRATION;

ANIMALS; DRUG EVALUATION, PRECLINICAL; ENZYME INHIBITORS; MAGNETIC RESONANCE SPECTROSCOPY; MICE; MICE, INBRED C57BL; PYRIDINES; SPECTROMETRY, MASS, ELECTROSPRAY IONIZATION; STEAROYL-COA DESATURASE; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 77957825925     PISSN: 02235234     EISSN: 17683254     Source Type: Journal    
DOI: 10.1016/j.ejmech.2010.07.044     Document Type: Article

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