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Volumn 22, Issue 1, 2012, Pages 623-627

Discovery of potent and liver-selective stearoyl-CoA desaturase (SCD) inhibitors in an acyclic linker series

Author keywords

Desaturation index; Liver selective; MK 8245; SCD inhibitors; Stearoyl CoA desaturase inhibitors

Indexed keywords

ACYL COENZYME A DESATURASE; MK 8245; OXYGENASE INHIBITOR; STEAROYL COENZYME A DESATURASE INHIBITOR; UNCLASSIFIED DRUG;

EID: 84655163806     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2011.10.070     Document Type: Article
Times cited : (13)

References (22)
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    • Lachance, N.; Li, C. S.; Leclerc, J.-P.; Ramtohul, Y. WO 2008/128335.
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    • 15N gHMBC and 1D NOESY.
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    • Rat microsomal assay conditions: Li, C. S.; Ramtohul, Y.; Huang, Z.; Lachance, N. WO 2006/130986.
    • Rat microsomal assay conditions: Li, C. S.; Ramtohul, Y.; Huang, Z.; Lachance, N. WO 2006/130986.
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    • 0-6 h = 1.0 μM h.
    • 0-6 h = 1.0 μM h.
  • 20
    • 84655172619 scopus 로고    scopus 로고
    • For comparison, the isoxazole ring-opened metabolite was observed at low level (4%) in vitro in rat hepatocytes with MK-8245.
    • For comparison, the isoxazole ring-opened metabolite was observed at low level (4%) in vitro in rat hepatocytes with MK-8245.
  • 21
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    • Compounds containing a 6-membered heterocycle ring pyridazine or pyrazine were less potent. Data unpublished.
    • Compounds containing a 6-membered heterocycle ring pyridazine or pyrazine were less potent. Data unpublished.
  • 22
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    • 3, Ar) were evaluated across numerous combinations of different tether lengths and various 5-membered ring heterocycles. Unpublished results.
    • 3, Ar) were evaluated across numerous combinations of different tether lengths and various 5-membered ring heterocycles. Unpublished results.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.