- 6-O-SUBSTITUTED KETOLIDES HAVING ANTIBACTERIAL ACTIVITY
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PROBLEM TO BE SOLVED: To provide 6-O-substituted ketolides with antibacterial activity, having acid stability and enhanced activity toward gram negative bacteria and macrolide resistant gram positive bacteria. SOLUTION: This invention provides 6-O-substituted erythromycin ketolide derivatives such as formula (II) and compositions comprising the compounds. [Y and Z together form a group X; X is ketone, hydroxyimino or the like; or, one of Y and Z is H and the other is hydrogen, hydroxy or the like; Ra is H, hydroxy; Rc is H or a hydroxy protective group; R is a substituted methyl group]. COPYRIGHT: (C)2015,JPOandINPIT
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- Process for the preparation of enantiomerically enriched compounds
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1. Process for the preparation of enantiomerically enriched amino aldehydes and amino alcohols, wherein a corresponding enantiomerically enriched amino nitrile is subjected to hydrogenation in the presence of hydrogen, a hydrogenation catalyst, preferably a Pd-catalyst and a mineral acid. For the preparation of an amino aldehyde hydrogen preferably is present at a hydrogen-pressure between 0.1 and 2 MPa, in particular between 0.5 and 1 MPa. The amino aldehyde preferably is isolated in the form of a chemically and configurationally stable derivative. For the preparation of an amino alcohol, preferably at least during part of the hydrogenation hydrogen is present at a hydrogen-pressure between 2 and 10 MPa, in particular between 4 and 6 MPa. In a preferred embodiment the hydrogen-pressure initially is between 0,5 and 2 MPa and subsequently, after most of the nitrile starting material is converted, the hydrogen pressure is increased to a value between 2 and 10 MPa. The enantiomerically enriched nitrile starting material may a.o. be prepared by enzymatic resolution, classical resolution, resolution via preferential crystallization, diastereomeric synthesis, catalytic asymmetric synthesis or dehydratation of amino acid amides.
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Page/Page column 6
(2010/11/29)
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- Macrolide antiinfective agents
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The invention is directed towards antibacterial compounds. The invention concerns macrolide antibiotics useful as antiinfective agents.
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- Tricyclic erythromycin derivatives
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Compounds, or pharmaceutically acceptable salts and esters thereof, of the formula: wherein A, B, D and E, R1, R2, and Z are specifically defined, having antibacterial activity, pharmaceutical compositions containing said compounds, treatment of bacterial infections with such compositions, and processes for the preparation of the compounds.
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- 6-O-substituted ketolides having antibacterial activity
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Antimicrobial compounds having the formula STR1 as well as pharmaceutically acceptable salts, esters or prodrugs thereof; pharmaceutical compositions comprising such compounds; methods of treating bacterial infections by the administration of such compounds; and processes for the preparation of the compounds.
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- Inhibition of cell growth and [3H]-thymidine incorporation in human mammary carcinoma cell line MDA-MB 231 by PtCi2-complexes of 1.2-diaminoethanes derived from amino acids
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Substituted L-1.2-diaminoethanes were prepared from L-α-amino acids and used as ligand in the synthesis of platinum(II) complexes. The L-1.2-diaminoethane-dichloro-platinum(II) complexes were examined with respect to their cytostatic effect. As an in vitro test system the hormone independent human mammary carcinoma cell line MDA-MB 231 was used. All the examined complexes cause a strong inhibition of DNA synthesis in the tumor cells.
- Brunner,Schmidt,Unger,Schonenberger
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p. 509 - 512
(2007/10/02)
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