当前位置： SCI文献检索 > EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY期刊下所有文献 > Aminopropylindenes derived from Grundmann's ketone as a novel chemotype of oxidosqualene cyclase inhibitors.

Aminopropylindenes derived from Grundmann's ketone as a novel chemotype of oxidosqualene cyclase inhibitors.

Abstract：

:A series of aminopropylindenes, designed as mimics of a cationic high energy intermediate in the oxidosqualene cyclase(1) (OSC)-mediated cyclization of 2,3-oxidosqualen to lanosterol was prepared from Grundmann's ketone. Screening on OSCs from five different organisms revealed interesting activities and selectivities of some of the compounds. A N,N-dimethylaminopropyl derivative showed promising inhibition of Trypanosoma cruzi OSC in combination with low cytotoxicity, and showed significant reduction of cholesterol biosynthesis in a human cell line.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Lange S,Keller M,Müller C,Oliaro-Bosso S,Balliano G,Bracher F

doi

10.1016/j.ejmech.2013.03.002

subject

Has Abstract

pub_date

2013-05-01 00:00:00

pages

758-64

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(13)00149-9

journal_volume

63

pub_type

杂志文章

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