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Volumn 15, Issue 23, 2005, Pages 5266-5269

Discovery of 4-heteroarylbicyclo[2.2.2]octyltriazoles as potent and selective inhibitors of 11β-HSD1: Novel therapeutic agents for the treatment of metabolic syndrome

Author keywords

11 HSD1; 11 HSD2; 11 Hydroxysteroid dehydrogenase type I; Bicyclo 2.2.2 octyltriazole; Cortisol; Cortisone; Glucocorticoids; Heterocycle; Imidazole; Metabolic syndrome; Oxadiazole; Pharmacodynamic assay; Pharmacokinectics; Triazole

Indexed keywords

11BETA HYDROXYSTEROID DEHYDROGENASE; TRIAZOLE DERIVATIVE;

EID: 26844460594     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2005.08.052     Document Type: Article
Times cited : (63)

References (18)
  • 13
    • 26844514613 scopus 로고    scopus 로고
    • note
    • For mouse and rat liver microsomal studies, parent compound (2 μM) was incubated in liver microsomal suspension (1 mg protein/mL of 0.1 M phosphate buffer containing 1 mM EDTA at pH 7.4) containing 5 mM NADPH at 37°C for 1 h. The major oxidative metabolite (hydroxylation of the ω-1 carbon on the 5-carbon alkyl chain) was biosynthesized via incubation of parent compound (2 mM) in recombinant rCYP-2C11 suspension (1 mg protein/mL) containing NADPH regenerating system at 37°C for 24 h. LC/MS and NMR were used to identify the structure of the metabolite (unpublished results).


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.