The discovery of 2-anilinothiazolones as 11beta-HSD1 inhibitors.

The discovery of 2-anilinothiazolones as 11beta-HSD1 inhibitors. Research Abstract Details 

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The discovery of 2-anilinothiazolones as 11beta-HSD1 inhibitors. Abstract Text:

Chester Yuan,David J St Jean,Qingyian Liu,Lynn Cai,Aiwen Li,Nianhe Han,George Moniz,Ben Askew,Randall W Hungate,Lars Johansson,Lars Tedenborg,David Pyring,Meredith Williams,Clarence Hale,Michelle Chen,Rod Cupples,Jiandong Zhang,Steven Jordan,Michael D Bartberger,Yaxiong Sun,Maurice Emery,Minghan Wang,Christopher Fotsch,

A series of 2-anilinothiazolones were prepared as inhibitors of 11beta-hydroxysteroid dehydrogenase type 1 (11beta-HSD1). The most potent compounds contained a 2-chloro or 2-fluoro group on the aniline ring with an isopropyl substituent on the 5-position of the thiazolone ring (compounds 2 and 3, respectively). The binding mode was determined through the X-ray co-crystal structure of the enzyme with compound 3. This compound was also approximately 70-fold selective over 11beta-HSD2 and was orally bioavailable in rat pharmacokinetic studies. However, compound 3 was >580-fold less active in the 11beta-HSD1 cell assay when tested in the presence of 3% human serum albumin.

The discovery of 2-anilinothiazolones as 11beta-HSD1 inhibitors. Publishing Authors By Initials

C Yuan,DJ St Jean,Q Liu,L Cai,A Li,N Han,G Moniz,B Askew,RW Hungate,L Johansson,L Tedenborg,D Pyring,M Williams,C Hale,M Chen,R Cupples,J Zhang,S Jordan,MD Bartberger,Y Sun,M Emery,M Wang,C Fotsch,

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The discovery of 2-anilinothiazolones as 11beta-HSD1 inhibitors. Journal Published:

PUBLICATION TYPE: Journal Article

Journal: Bioorganic & medicinal chemistry letters

VOLUME: 17

Page Numbers: 6056-61

Journal Abbreviation: Bioorg. Med. Chem. Lett.

ISSN: 0960-894X

DAY: 25

MONTH: 09

YEAR: 2007

The discovery of 2-anilinothiazolones as 11beta-HSD1 inhibitors. Information

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LANGUAGE: eng

NlmUniqueID: 9107377

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Grant and Affiliation Information for The discovery of 2-anilinothiazolones as 11beta-HSD1 inhibitors.

AFFILIATION: Amgen Inc., Thousand Oaks, CA 91320, USA.

Country: England

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MEDLINETA: Bioorg Med Chem Lett

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ACCESSION NUMBER: 2RBE

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