当前位置： SCI文献检索 > BIOORGANIC & MEDICINAL CHEMISTRY LETTERS期刊下所有文献 > Discovery and structure-guided drug design of inhibitors of 11beta-hydroxysteroid-dehydrogenase type I based on a spiro-carboxamide scaffold.

Discovery and structure-guided drug design of inhibitors of 11beta-hydroxysteroid-dehydrogenase type I based on a spiro-carboxamide scaffold.

Abstract：

:Spiro-carboxamides were identified as inhibitors of 11beta-hydroxysteroid-dehydrogenase type 1 by high-throughput screening. Structure-based drug design was used to optimise the initial hit yielding a sub-nanomolar IC(50) inhibitor (0.5nM) on human 11beta-HSD1 with a high binding efficiency index (BEI of 32.7) which was selective against human 11beta-HSD2 (selectivity ratio>200000).

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Lepifre F,Christmann-Franck S,Roche D,Leriche C,Carniato D,Charon C,Bozec S,Doare L,Schmidlin F,Lecomte M,Valeur E

doi

10.1016/j.bmcl.2009.02.123

subject

Has Abstract

pub_date

2009-07-01 00:00:00

pages

3682-5

issue

13

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(09)00291-1

journal_volume

19

pub_type

杂志文章

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