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
- 239000003814 drug Substances 0.000 title abstract 2
- 239000003242 anti bacterial agent Substances 0.000 abstract 5
- 229940088710 antibiotic agent Drugs 0.000 abstract 5
- 239000013543 active substance Substances 0.000 abstract 3
- 230000001580 bacterial effect Effects 0.000 abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 3
- XEEYBQQBJWHFJM-UHFFFAOYSA-N Iron Chemical compound [Fe] XEEYBQQBJWHFJM-UHFFFAOYSA-N 0.000 abstract 2
- 239000000589 Siderophore Substances 0.000 abstract 2
- 239000002253 acid Substances 0.000 abstract 2
- YCIMNLLNPGFGHC-UHFFFAOYSA-N catechol Chemical compound OC1=CC=CC=C1O YCIMNLLNPGFGHC-UHFFFAOYSA-N 0.000 abstract 2
- UXTZUUVTGMDXNG-UHFFFAOYSA-N 1,2-benzoxazine-3,4-dione Chemical class C1=CC=C2C(=O)C(=O)NOC2=C1 UXTZUUVTGMDXNG-UHFFFAOYSA-N 0.000 abstract 1
- 241000588724 Escherichia coli Species 0.000 abstract 1
- -1 R2 represents H Chemical group 0.000 abstract 1
- 241000607142 Salmonella Species 0.000 abstract 1
- 150000007513 acids Chemical class 0.000 abstract 1
- 125000000217 alkyl group Chemical group 0.000 abstract 1
- 150000001413 amino acids Chemical class 0.000 abstract 1
- 230000000844 anti-bacterial effect Effects 0.000 abstract 1
- 125000004181 carboxyalkyl group Chemical group 0.000 abstract 1
- 239000002738 chelating agent Substances 0.000 abstract 1
- 229940079593 drug Drugs 0.000 abstract 1
- 150000002148 esters Chemical class 0.000 abstract 1
- 125000000623 heterocyclic group Chemical group 0.000 abstract 1
- 150000007857 hydrazones Chemical class 0.000 abstract 1
- 229910052742 iron Inorganic materials 0.000 abstract 1
- 230000010438 iron metabolism Effects 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 102000004196 processed proteins & peptides Human genes 0.000 abstract 1
- 108090000765 processed proteins & peptides Proteins 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
Landscapes
- 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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