4-Methyl-5-phenyl triazoles as selective inhibitors of 11β-hydroxysteroid dehydrogenase type I

Yuping Zhu; Steven H. Olson; Anne Hermanowski-Vosatka; Steven Mundt; Kashmira Shah; Marty Springer; Rolf Thieringer; Samuel Wright; Jianying Xiao; Hratch Zokian; James M. Balkovec

doi:10.1016/j.bmcl.2008.04.013

4-Methyl-5-phenyl triazoles as selective inhibitors of 11β-hydroxysteroid dehydrogenase type I

Yuping Zhu
, Steven H. Olson
, Anne Hermanowski-Vosatka
, Steven Mundt
, Kashmira Shah
, Marty Springer
, Rolf Thieringer
, Samuel Wright
, Jianying Xiao
, Hratch Zokian
, James M. Balkovec

Center for Discovery and Innovation

Merck

Research output: Contribution to journal › Article › peer-review

34 Scopus citations

Abstract

4-Methyl-5-phenyl-(1,2,4)-triazoles were identified as selective inhibitors of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1). They were active in vitro and in an in vivo mouse pharmacodynamic (PD) model. The synthesis and structure activity relationships are presented.

Original language	English
Pages (from-to)	3405-3411
Number of pages	7
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	18
Issue number	11
DOIs	https://doi.org/10.1016/j.bmcl.2008.04.013
State	Published - 1 Jun 2008

Keywords

11β-HSD1
4-Methyl-5-phenyl triazole
Metabolic syndrome

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10.1016/j.bmcl.2008.04.013

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title = "4-Methyl-5-phenyl triazoles as selective inhibitors of 11β-hydroxysteroid dehydrogenase type I",

abstract = "4-Methyl-5-phenyl-(1,2,4)-triazoles were identified as selective inhibitors of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1). They were active in vitro and in an in vivo mouse pharmacodynamic (PD) model. The synthesis and structure activity relationships are presented.",

keywords = "11β-HSD1, 4-Methyl-5-phenyl triazole, Metabolic syndrome",

author = "Yuping Zhu and Olson, \{Steven H.\} and Anne Hermanowski-Vosatka and Steven Mundt and Kashmira Shah and Marty Springer and Rolf Thieringer and Samuel Wright and Jianying Xiao and Hratch Zokian and Balkovec, \{James M.\}",

year = "2008",

month = jun,

day = "1",

doi = "10.1016/j.bmcl.2008.04.013",

language = "English",

volume = "18",

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journal = "Bioorganic and Medicinal Chemistry Letters",

issn = "0960-894X",

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TY - JOUR

T1 - 4-Methyl-5-phenyl triazoles as selective inhibitors of 11β-hydroxysteroid dehydrogenase type I

AU - Zhu, Yuping

AU - Olson, Steven H.

AU - Hermanowski-Vosatka, Anne

AU - Mundt, Steven

AU - Shah, Kashmira

AU - Springer, Marty

AU - Thieringer, Rolf

AU - Wright, Samuel

AU - Xiao, Jianying

AU - Zokian, Hratch

AU - Balkovec, James M.

PY - 2008/6/1

Y1 - 2008/6/1

N2 - 4-Methyl-5-phenyl-(1,2,4)-triazoles were identified as selective inhibitors of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1). They were active in vitro and in an in vivo mouse pharmacodynamic (PD) model. The synthesis and structure activity relationships are presented.

AB - 4-Methyl-5-phenyl-(1,2,4)-triazoles were identified as selective inhibitors of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1). They were active in vitro and in an in vivo mouse pharmacodynamic (PD) model. The synthesis and structure activity relationships are presented.

KW - 11β-HSD1

KW - 4-Methyl-5-phenyl triazole

KW - Metabolic syndrome

UR - https://www.scopus.com/pages/publications/44149092411

U2 - 10.1016/j.bmcl.2008.04.013

DO - 10.1016/j.bmcl.2008.04.013

M3 - Article

C2 - 18440811

AN - SCOPUS:44149092411

SN - 0960-894X

VL - 18

SP - 3405

EP - 3411

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 11

ER -

4-Methyl-5-phenyl triazoles as selective inhibitors of 11β-hydroxysteroid dehydrogenase type I

Abstract

Keywords

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