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Volumn 18, Issue 14, 2008, Pages 4224-4227

Discovery of a potent, selective, and less flexible selective norepinephrine reuptake inhibitor (sNRI)

Author keywords

Norepinephrine; Serotonin

Indexed keywords

ATOMOXETINE; DESIPRAMINE; DULOXETINE; FLUOXETINE; NBI 80532; NISOXETINE; NORADRENALIN TRANSPORTER; NORADRENALIN UPTAKE INHIBITOR; REBOXETINE;

EID: 47149097253     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2008.05.057     Document Type: Article
Times cited : (22)

References (20)
  • 7
    • 47149112976 scopus 로고    scopus 로고
    • Mackay, M. Pfizer R&D Analyst Meeting 2006, Neurosciences slide 9, http://www.pfizer.com/investors/presentations/presentations.jsp, web site accessed 5/2008.
    • Mackay, M. Pfizer R&D Analyst Meeting 2006, Neurosciences slide 9, http://www.pfizer.com/investors/presentations/presentations.jsp, web site accessed 5/2008.
  • 15
    • 47149102744 scopus 로고    scopus 로고
    • note
    • Compound 9c was crystalline and easily separated from the trans oil 9t by crystallization.
  • 17
    • 47149093005 scopus 로고    scopus 로고
    • Kiankarimi, M.; Hudson, S.; Dwight, W. J.; Wade, W. S. Preparation of benzofuranylmethylamines, chromanylmethylamines, and thiochromanylmethylamines as monoamine reuptake inhibitors. US 2006252818.
    • Kiankarimi, M.; Hudson, S.; Dwight, W. J.; Wade, W. S. Preparation of benzofuranylmethylamines, chromanylmethylamines, and thiochromanylmethylamines as monoamine reuptake inhibitors. US 2006252818.
  • 18
    • 47149099384 scopus 로고    scopus 로고
    • note
    • 3-d) δ ppm 9.84 (s, 1H), 9.67 (s, 1H), 7.30 (t, J = 7 Hz, 1H), 7.20 (m, 3H), 7.16 (d, J = 7 Hz, 1H), 7.15 (t, J = 7 Hz, 1H), 7.04 (d, J = 8 Hz, 1H), 6.94 (t, J = 7 Hz, 1H), 5.45 (s, 1H), 3.77 (s, 1H), 3.40 (dd, J = 15, 4 Hz, 1H), 3.05 (dd, J = 15, 12 Hz, 1H), 2.72 (s, 3H) 2.14 (t, J = 12 Hz, 1H), 2.04 (s, 3H); APCI MS m/z 268.0.
  • 19
    • 47149094681 scopus 로고    scopus 로고
    • note
    • Molecule structures were imported into the Molecular Operating Environment (MOE) software version 2007.09 and subjected to Stochastic Conformation Search using the MMFF94x force field with GBSA implicit solvation. Low-energy conformations within 1.5 kcal/mol from the minimum that were most consistent with the known solid-state X-ray crystal structures were taken forward and aligned using the Flexible Alignment module using default field similarity terms except hydrogen-bonding terms were scaled down to 0.5. The best scoring alignment most consistent with known structure-activity patterns for NET:SERT selectivity was retained.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.