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Volumn 15, Issue 19, 2005, Pages 4359-4362

Adamantyl triazoles as selective inhibitors of 11β-hydroxysteroid dehydrogenase type 1

Author keywords

11 HSD1; Adamantyl triazole; Metabolic syndrome

Indexed keywords

11BETA HYDROXYSTEROID DEHYDROGENASE; 11BETA HYDROXYSTEROID DEHYDROGENASE 1; ADAMANTANE DERIVATIVE; OXIDOREDUCTASE INHIBITOR; TRIAZOLE DERIVATIVE; UNCLASSIFIED DRUG;

EID: 23944454884     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2005.06.040     Document Type: Article
Times cited : (103)

References (34)
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    • Metabolism 15 2004 418
    • (2004) Metabolism , vol.15 , pp. 418
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    • N.J. Goulding P.J. Flower Birkhëuser Switzerland
    • M.B. Feinstein, and R.P. Schleimer N.J. Goulding P.J. Flower Glucocorticoids 2001 Birkhëuser Switzerland 147 158
    • (2001) Glucocorticoids , pp. 147-158
    • Feinstein, M.B.1    Schleimer, R.P.2
  • 27
    • 33645393270 scopus 로고    scopus 로고
    • note
    • The in vitro enzymatic activity was assessed via a scintillation proximity assay (SPA). Tritiated-cortisone, NADPH, and test compound were incubated with 11β-HSD1 from CHO transfectants at 37°C to allow conversion to cortisol to progress. Following incubation, a preparation of protein A-coated SPA beads, pre-blended with anti-cortisol monoclonal antibody MAb and a nonspecific 11β-HSD1 inhibitor (18β-glycyrrhetinic acid), was added to each well. The mixture was read on a scintillation counter. This is similar to the method described in Ref. 8a.
  • 30
    • 0031953654 scopus 로고    scopus 로고
    • Noncommercial hydrazides were best prepared on small scale from the corresponding acid following the procedure of U. Boas, B. Pedersen, and J.B. Christensen Synth. Commun. 28 1998 1223 On large scale, the methyl ester was heated with excess hydrazine to provide the hydrazide in good yield
    • (1998) Synth. Commun. , vol.28 , pp. 1223
    • Boas, U.1    Pedersen, B.2    Christensen, J.B.3
  • 32
    • 33645406995 scopus 로고    scopus 로고
    • note
    • Prepared by the reaction of 14 with (diethylamino)sulfur trifluoride (DAST) in dichloromethane at room temperature.
  • 33
    • 84981833838 scopus 로고
    • (3,5-Dimethyl-1-adamantyl)acetic acid was prepared by the method of K. Bott Chem. Ber. 101 1968 564
    • (1968) Chem. Ber. , vol.101 , pp. 564
    • Bott, K.1


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.