[EN] NOVEL CYSTOBACTAMIDE DERIVATIVES<br/>[FR] NOUVEAUX DÉRIVÉS DE CYSTOBACTAMIDES
申请人:HELMHOLTZ ZENTRUM INFEKTIONSFORSCHUNG GMBH
公开号:WO2019038405A1
公开(公告)日:2019-02-28
The present invention relates to novel derivatives of cystobactamides of formula (lb) and the use thereof for the treatment or prophylaxis of bacterial infections.
申请人:HELMHOLTZ-ZENTRUM FÜR INFEKTIONSFORSCHUNG GMBH
公开号:US11034648B2
公开(公告)日:2021-06-15
The present invention relates to novel derivatives of cystobactamides of formula (Ib) and the use thereof for the treatment or prophylaxis of bacterial infections.
Axially chiral bis(salicylidene)ethylenediamine (H(2)salen)-type ligands 3 (cf: Schemes 1 and 3) are efficient ligands for the enantioselective addition of diethylzinc to aldehydes. There is ample evidence that an active bimetallic catalyst forms an effective chiral pocket (see Fig.2); of a series of first-row transition-metal complexes with these ligands, the most stereoselective were the Co-II complexes (see Fig. I). Best ee values as well as the fastest rates (see Tables 2 and 3) were obtained with these Co-II complexes when an EtO substituent was present at C(3) of the salicylaldehyde residues of ligand 3 (R-1 = EtO), Le., complex [Co-II(3'h)] produced up to 93% ee with aromatic aldehydes and 78% ee for aliphatic aldehydes (see Table 4).
NOVEL CYSTOBACTAMIDE DERIVATIVES
申请人:Helmholtz-Zentrum für Infektionsforschung GmbH