Armeniaspiroles, a novel class of natural products isolated from Streptomyces armeniacus, are characterized by a novel spiro[4.4]non-8-ene scaffold. Various derivatives of Armeniaspiroles could be obtained by halogenation, alkylation, addition/elimination or reductions. A total synthesis of the 5-chloro analog of Armeniaspirole A has been accomplished in a linear six-step sequence. 5-Chloro-Armeniaspirole A exhibits good activity against a range of multidrug-resistant, Gram-positive bacterial pathogens. (C) 2012 Elsevier Ltd. All rights reserved.
STREPTOSPIROLE DERIVATIVES
申请人:Dufour-Schroif Cosima
公开号:US20110295009A1
公开(公告)日:2011-12-01
The invention relates to streptospirole derivatives of the general formula (I), wherein R
1
, R
2
, R
3
, X
1
, X
2
, Y
1
and Y
2
are as defined herein, a process for the preparation of said compounds by fermenting the microorganism
Streptomyces
sp. ST 108140 (DSM 19369) and optionally derivatizing the compounds produced by said microorganism, a pharmaceutical composition comprising at least one compound of the formula (I), and the use of a compound of the formula (I) for the preparation of a medicament for the treatment and/or prophylaxis of bacterial infections.