Modulation of 11beta-hydroxysteroid dehydrogenase type 1 activity by 1,5-substituted 1H-tetrazoles.
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ABSTRACT:
SUBMITTER: Webster SP
PROVIDER: S-EPMC3972730 | biostudies-literature | 2010 Jun
REPOSITORIES: biostudies-literature
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Modulation of 11beta-hydroxysteroid dehydrogenase type 1 activity by 1,5-substituted 1H-tetrazoles.
Webster Scott P SP Binnie Margaret M McConnell Kirsty M M KM Sooy Karen K Ward Peter P Greaney Michael F MF Vinter Andy A Pallin T David TD Dyke Hazel J HJ Gill Matthew I A MI Warner Ines I Seckl Jonathan R JR Walker Brian R BR
Bioorganic & medicinal chemistry letters 20100418 11
Inhibitors of 11beta-hydroxysteroid dehydrogenase (11beta-HSD1) show promise as drugs to treat metabolic disease and CNS disorders such as cognitive impairment. A series of 1,5-substituted 1H-tetrazole 11beta-HSD1 inhibitors has been discovered and chemically modified. Compounds are selective for 11beta-HSD1 over 11beta-HSD2 and possess good cellular potency in human and murine 11beta-HSD1 assays. A range of in vitro stabilities are observed in human liver microsome assays. ...[more]
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