FIELD: chemistry.
SUBSTANCE: invention relates to the N" -substituted 9a-N-(N'- carbamoyl-γ-aminopropyl) and 9a-M-(M'-thiocarbamoyl-γ-aminopropyl)) derivatives of 9-desoxo-9-dihydro-9a-ase-9a-homoerythromycine A or 5-O-desosaminyl-9-desoxo-9-dihydro-9a-ase-9a-homoerythronolide A, novel semisynthetic macrolide antibiotics from the group of azalides with the common formula 1, where R means H or cladinosyl fragment, R means H, R means the isopropyl group, 1-naphtyl, 2-naphtyl, benzene, 2-(trifluoromethyl)phenyl, 3-phenylpropyl, (3-phenylethyl, ehtoxicarbonylmethyl, 1-(1-naphtyl)ethyl, 3,4,5-trimethoxiphenyl and 2,4-dichlorphenyl, and X means O or S, or to their pharmaceutically compliant additive salts with the inorganic or organic acids and to the method of their production. The invention also relates to the pharmaceutical composition with the antibacterial activity and to the application of the compounds with the common formula 1 or their pharmaceutically compliant salts, in producing the said composition.
EFFECT: antibacterial activity.
16 cl, 26 ex, 1 tbl
Title | Year | Author | Number |
---|---|---|---|
9A-N-[N'-(PHENYLSULFONYL)CARBAMOYL]-DERIVATIVES OF 9-DEOXO-9-DIHYDRO-9A-AZA-9A-HOMOERYTHROMYCIN A AND 5-DESOSAMINYL-9-DEOXO-9-DIHYDRO-9A-AZA-9A-HOMOERYTHRONOLIDE A, METHOD FOR THEIR PREPARING AND PHARMACEUTICAL COMPOSITION BASED ON THEREOF | 2002 |
|
RU2270836C2 |
9A-N-(N'-CARBAMOYL)- OR 9A-N-(N'-THIOCARBANOYL)-DERIVATIVES OF 9-DEOXO-9A-AZA-9A-HOMOERYTHROMYCIN A, METHOD OF THEIR SYNTHESIS AND PHARMACEUTICAL COMPOSITION BASED ON SAID | 1994 |
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RU2131878C1 |
β, β-DISUBSTITUTED DERIVATIVES OF 9-DEOXO-9A-N-ETHENYL-9A-AZA-9A- HOMOERYTHROMYCIN A | 1998 |
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NEW KETOAZOLIDES AND METHOD FOR THEIR PREPARING | 1999 |
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RU2211222C2 |
9A-AZALIDE FRAGMENTS OF MACROLIDE ANTIBIOTICS OF AZALIDE CLASS, METHOD OF THEIR SYNTHESIS AND INTERMEDIATE COMPOUNDS FOR THEIR SYNTHESIS | 1995 |
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MACROLIDE DERIVATIVES | 2007 |
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PROCESS FOR PREPARING 9-DESOXY-9A-METHYLENEISOSTERS PGI 2 OR THEIR LACTONES OR SALTS | 0 |
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2,3-DIHYDRO-1H-INDEN-1-YL-2,7-DIAZASPIRO[3,5]NONANE DERIVATIVES AND USE THEREOF AS GHRELIN RECEPTOR ANTAGONISTS OR INVERSE AGONISTS | 2011 |
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METHOD OF PRODUCING 9-DIOXI-9A-METHYLENE ISOSTERS OR THEIR LACTONES | 0 |
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RU2808572C2 |
Authors
Dates
2008-07-10—Published
2003-12-10—Filed