ECSP982439A - DERIVATIVES OF BENZOXAZINDIONA, APPLICATION OF THE SAME AND MEDICINES THAT CONTAIN THEM - Google Patents
DERIVATIVES OF BENZOXAZINDIONA, APPLICATION OF THE SAME AND MEDICINES THAT CONTAIN THEMInfo
- Publication number
- ECSP982439A ECSP982439A ECSP982439A ECSP982439A EC SP982439 A ECSP982439 A EC SP982439A EC SP982439 A ECSP982439 A EC SP982439A EC SP982439 A ECSP982439 A EC SP982439A
- Authority
- EC
- Ecuador
- Prior art keywords
- antibiotics
- compounds
- derivatives
- siderophores
- conjugates
- Prior art date
Links
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- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
La invención se refiere a novedosos derivados de benzoxazindiona de la fórmula general I, y sus conjugados con sustancia activa, por ejemplo antibióticos. Los compuestos de la presente invención constituyen derivados heterocíclicos protegidos de catecol y son eficaces como sideróforos frente a cepas bacterianas gram negativas, particularmente Pseudomonáceas, cepas E.coli y Salmonella. Los mismos en forma de us conjugados con sustancia activas, por ejemplo antibióticos (conjugados antibióticos sideróforos) pueden introducir estos antibióticos en la célula bacteriana y aumentar o ampliar su eficacia antibacteriana en parte también frente a otras cepas bacterianas resistentes a otras B-lactamas. Además dichos compuestos son adecuados como formas premedicamentosas potenciales como quelatantes del hierro para la utilización en afecciones causadas por perturbaciones de metabolismo del hierro. La aplicación de la invención puede tener lugar en investigación farmacéutica, industria y agricultura. Fórmula I (gráfico), en donde R1 representa H o carboxialquilo, R2 representa H, alquilo o fenilo y R3 representa diversos grupos ácidos derivados de aminoácidos, depéptidos e hidrazonas o sus conjugados con sustancias activas, por ejemplo antibióticos. Dichos compuestos pueden existir en forma de ácidos libres, de sus sales o como ésteres fácilmente desdoblables.The invention relates to novel benzoxazindione derivatives of the general formula I, and their conjugates with active substance, for example antibiotics. The compounds of the present invention constitute catechol protected heterocyclic derivatives and are effective as siderophores against gram negative bacterial strains, particularly Pseudomonaceae, E.coli strains and Salmonella. The same in the form of us conjugated with active substances, for example antibiotics (conjugated antibiotics siderophores) can introduce these antibiotics into the bacterial cell and increase or extend their antibacterial efficacy in part also against other bacterial strains resistant to other B-lactams. Furthermore such compounds are suitable as potential pre-drug forms as iron chelators for use in conditions caused by disturbances of iron metabolism. The application of the invention can take place in pharmaceutical research, industry and agriculture. Formula I (graph), wherein R1 represents H or carboxyalkyl, R2 represents H, alkyl or phenyl and R3 represents various acid groups derived from amino acids, peptides and hydrazones or their conjugates with active substances, for example antibiotics. Said compounds can exist in the form of free acids, their salts or as easily cleavable esters.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| ECSP982439 ECSP982439A (en) | 1998-03-04 | 1998-03-04 | DERIVATIVES OF BENZOXAZINDIONA, APPLICATION OF THE SAME AND MEDICINES THAT CONTAIN THEM |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| ECSP982439 ECSP982439A (en) | 1998-03-04 | 1998-03-04 | DERIVATIVES OF BENZOXAZINDIONA, APPLICATION OF THE SAME AND MEDICINES THAT CONTAIN THEM |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ECSP982439A true ECSP982439A (en) | 1999-01-19 |
Family
ID=42043361
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ECSP982439 ECSP982439A (en) | 1998-03-04 | 1998-03-04 | DERIVATIVES OF BENZOXAZINDIONA, APPLICATION OF THE SAME AND MEDICINES THAT CONTAIN THEM |
Country Status (1)
| Country | Link |
|---|---|
| EC (1) | ECSP982439A (en) |
-
1998
- 1998-03-04 EC ECSP982439 patent/ECSP982439A/en unknown
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