Discovery and biological evaluation of adamantyl amide 11beta-HSD1 inhibitors

Scott P Webster; Peter Ward; Margaret Binnie; Eilidh Craigie; Kirsty M M McConnell; Karen Sooy; Andy Vinter; Jonathan R Seckl; Brian R Walker

doi:10.1016/j.bmcl.2007.02.057

Discovery and biological evaluation of adamantyl amide 11beta-HSD1 inhibitors

Scott P Webster, Peter Ward, Margaret Binnie, Eilidh Craigie, Kirsty M M McConnell, Karen Sooy, Andy Vinter, Jonathan R Seckl, Brian R Walker

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

Abstract

A series of adamantyl amide 11beta-HSD1 inhibitors has been discovered and chemically modified. Selected compounds are selective for 11beta-HSD1 over 11beta-HSD2 and possess excellent cellular potency in human and murine 11beta-HSD1 assays. Good pharmacodynamic characteristics are observed in ex vivo assays.

Original language	English
Pages (from-to)	2838-2843
Number of pages	6
Journal	Bioorganic & Medicinal Chemistry Letters
Volume	17
Issue number	10
DOIs	https://doi.org/10.1016/j.bmcl.2007.02.057
Publication status	Published - 15 May 2007

Keywords

Metabolic syndrome
11β-HSD1
11β-HSD2
Inhibitor
Adamantane
Amide
Diabetes
11β-Hydroxysteroid dehydrogenase
Enzyme inhibition
Hsd1

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10.1016/j.bmcl.2007.02.057

http://www.sciencedirect.com/science/article/pii/S0960894X07002545

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title = "Discovery and biological evaluation of adamantyl amide 11beta-HSD1 inhibitors",

abstract = "A series of adamantyl amide 11beta-HSD1 inhibitors has been discovered and chemically modified. Selected compounds are selective for 11beta-HSD1 over 11beta-HSD2 and possess excellent cellular potency in human and murine 11beta-HSD1 assays. Good pharmacodynamic characteristics are observed in ex vivo assays.",

keywords = "Metabolic syndrome , 11β-HSD1 , 11β-HSD2 , Inhibitor , Adamantane , Amide , Diabetes , 11β-Hydroxysteroid dehydrogenase , Enzyme inhibition , Hsd1 ",

author = "Webster, {Scott P} and Peter Ward and Margaret Binnie and Eilidh Craigie and McConnell, {Kirsty M M} and Karen Sooy and Andy Vinter and Seckl, {Jonathan R} and Walker, {Brian R}",

year = "2007",

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doi = "10.1016/j.bmcl.2007.02.057",

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T1 - Discovery and biological evaluation of adamantyl amide 11beta-HSD1 inhibitors

AU - Webster, Scott P

AU - Ward, Peter

AU - Binnie, Margaret

AU - Craigie, Eilidh

AU - McConnell, Kirsty M M

AU - Sooy, Karen

AU - Vinter, Andy

AU - Seckl, Jonathan R

AU - Walker, Brian R

PY - 2007/5/15

Y1 - 2007/5/15

N2 - A series of adamantyl amide 11beta-HSD1 inhibitors has been discovered and chemically modified. Selected compounds are selective for 11beta-HSD1 over 11beta-HSD2 and possess excellent cellular potency in human and murine 11beta-HSD1 assays. Good pharmacodynamic characteristics are observed in ex vivo assays.

AB - A series of adamantyl amide 11beta-HSD1 inhibitors has been discovered and chemically modified. Selected compounds are selective for 11beta-HSD1 over 11beta-HSD2 and possess excellent cellular potency in human and murine 11beta-HSD1 assays. Good pharmacodynamic characteristics are observed in ex vivo assays.

KW - Metabolic syndrome

KW - 11β-HSD1

KW - 11β-HSD2

KW - Inhibitor

KW - Adamantane

KW - Amide

KW - Diabetes

KW - 11β-Hydroxysteroid dehydrogenase

KW - Enzyme inhibition

KW - Hsd1

U2 - 10.1016/j.bmcl.2007.02.057

DO - 10.1016/j.bmcl.2007.02.057

M3 - Article

C2 - 17350260

VL - 17

SP - 2838

EP - 2843

JO - Bioorganic & Medicinal Chemistry Letters

JF - Bioorganic & Medicinal Chemistry Letters

SN - 0960-894X

IS - 10

ER -

Discovery and biological evaluation of adamantyl amide 11beta-HSD1 inhibitors

Abstract

Keywords

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