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Design, synthesis, and biological evaluation of new (2E,6E)-10-(dimethylamino)-3,7-dimethyl-2,6-decadien-1-ol ethers as inhibitors of human and Trypanosoma cruzi oxidosqualene cyclase.

Authors :
Galli U
Oliaro-Bosso S
Taramino S
Venegoni S
Pastore E
Tron GC
Balliano G
Viola F
Sorba G
Source :
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2007 Jan 01; Vol. 17 (1), pp. 220-4. Date of Electronic Publication: 2006 Oct 05.
Publication Year :
2007

Abstract

New dimethylamino truncated squalene ether derivatives containing a different aromatic moiety (phenyl, naphthyl, and biphenyl) or a simple alkyl (n-hexylic) group were synthesized as inhibitors of the oxidosqualene cyclase (OSC) and of the sterol biosynthetic pathway. The activity against human OSC was compared with the activity against the OSCs of pathogenic organisms such as Pneumocystis carinii and Trypanosoma cruzi. The phenyl derivative was the most potent inhibitor of T. cruzi OSC.

Details

Language :
English
ISSN :
0960-894X
Volume :
17
Issue :
1
Database :
MEDLINE
Journal :
Bioorganic & medicinal chemistry letters
Publication Type :
Academic Journal
Accession number :
17027267
Full Text :
https://doi.org/10.1016/j.bmcl.2006.09.058