BR112015026362A2 - conjugados antibacterianos de sideróforo-aminopenicilina - Google Patents
conjugados antibacterianos de sideróforo-aminopenicilinaInfo
- Publication number
- BR112015026362A2 BR112015026362A2 BR112015026362A BR112015026362A BR112015026362A2 BR 112015026362 A2 BR112015026362 A2 BR 112015026362A2 BR 112015026362 A BR112015026362 A BR 112015026362A BR 112015026362 A BR112015026362 A BR 112015026362A BR 112015026362 A2 BR112015026362 A2 BR 112015026362A2
- Authority
- BR
- Brazil
- Prior art keywords
- conjugates
- siderophore
- aminopenicillin
- antibacterial
- catecholate
- Prior art date
Links
- 230000000844 anti-bacterial effect Effects 0.000 title abstract 2
- XEEYBQQBJWHFJM-UHFFFAOYSA-N Iron Chemical compound [Fe] XEEYBQQBJWHFJM-UHFFFAOYSA-N 0.000 abstract 4
- 239000000589 Siderophore Substances 0.000 abstract 2
- 230000001580 bacterial effect Effects 0.000 abstract 2
- 229940079593 drug Drugs 0.000 abstract 2
- 239000003814 drug Substances 0.000 abstract 2
- 229910052742 iron Inorganic materials 0.000 abstract 2
- 241000894006 Bacteria Species 0.000 abstract 1
- 229960003022 amoxicillin Drugs 0.000 abstract 1
- LSQZJLSUYDQPKJ-NJBDSQKTSA-N amoxicillin Chemical compound C1([C@@H](N)C(=O)N[C@H]2[C@H]3SC([C@@H](N3C2=O)C(O)=O)(C)C)=CC=C(O)C=C1 LSQZJLSUYDQPKJ-NJBDSQKTSA-N 0.000 abstract 1
- 229960000723 ampicillin Drugs 0.000 abstract 1
- AVKUERGKIZMTKX-NJBDSQKTSA-N ampicillin Chemical compound C1([C@@H](N)C(=O)N[C@H]2[C@H]3SC([C@@H](N3C2=O)C(O)=O)(C)C)=CC=CC=C1 AVKUERGKIZMTKX-NJBDSQKTSA-N 0.000 abstract 1
- 230000003115 biocidal effect Effects 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- 238000000338 in vitro Methods 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- LSQZJLSUYDQPKJ-UHFFFAOYSA-N p-Hydroxyampicillin Natural products O=C1N2C(C(O)=O)C(C)(C)SC2C1NC(=O)C(N)C1=CC=C(O)C=C1 LSQZJLSUYDQPKJ-UHFFFAOYSA-N 0.000 abstract 1
- 241000894007 species Species 0.000 abstract 1
Classifications
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
- A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
- A61K31/235—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids having an aromatic ring attached to a carboxyl group
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- A61K31/13—Amines
- A61K31/133—Amines having hydroxy groups, e.g. sphingosine
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- A61K31/16—Amides, e.g. hydroxamic acids
- A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
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- A61K31/16—Amides, e.g. hydroxamic acids
- A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
- A61K31/167—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
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- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
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- A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
- A61K31/404—Indoles, e.g. pindolol
- A61K31/405—Indole-alkanecarboxylic acids; Derivatives thereof, e.g. tryptophan, indomethacin
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- A61K31/407—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with other heterocyclic ring systems, e.g. ketorolac, physostigmine
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- A61K31/4196—1,2,4-Triazoles
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- A61K31/425—Thiazoles
- A61K31/429—Thiazoles condensed with heterocyclic ring systems
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- A61K31/439—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom the ring forming part of a bridged ring system, e.g. quinuclidine
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- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
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- A61K31/545—Compounds containing 5-thia-1-azabicyclo [4.2.0] octane ring systems, i.e. compounds containing a ring system of the formula:, e.g. cephalosporins, cefaclor, or cephalexine
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- A61K31/7036—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin having at least one amino group directly attached to the carbocyclic ring, e.g. streptomycin, gentamycin, amikacin, validamycin, fortimicins
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- A61K47/547—Chelates, e.g. Gd-DOTA or Zinc-amino acid chelates; Chelate-forming compounds, e.g. DOTA or ethylenediamine being covalently linked or complexed to the pharmacologically- or therapeutically-active agent
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Abstract
resumo conjugados antibacterianos de sideróforo-aminopenicilina foram sintetizados um sideróforo artificial do tipo tris-catecolato com uma estrutura principal tripodal e seu conjugado com ampicilina e amoxicilina. ambos os conjugados apresentaram atividades bacterianas in vitro significativamente potencializadas contra espécies gram-negativas em comparação a drogas de origem, principalmente contra p. aeruginosa. os conjugados parecem ser assimilados por um processo bacteriano de transporte de ferro induzido, já que suas atividades estavam inversamente relacionadas à concentração de ferro. os sideróforos do tipo tris-catecolato facilmente sintetizados podem ser usados com uma variedade de drogas como conjugados para se direcionarem a bactérias gram-negativas resistentes a antibiótico. 1/1
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US13/865,801 US9302012B2 (en) | 2012-04-18 | 2013-04-18 | Anti-bacterial siderophore-aminopenicillin conjugates |
PCT/US2013/066408 WO2014171971A1 (en) | 2013-04-18 | 2013-10-23 | Anti-bacterial siderophore-aminopenicillin conjugates |
Publications (1)
Publication Number | Publication Date |
---|---|
BR112015026362A2 true BR112015026362A2 (pt) | 2017-07-25 |
Family
ID=49380670
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
BR112015026362A BR112015026362A2 (pt) | 2013-04-18 | 2013-10-23 | conjugados antibacterianos de sideróforo-aminopenicilina |
Country Status (12)
Country | Link |
---|---|
US (1) | US9302012B2 (pt) |
EP (1) | EP2986617A4 (pt) |
JP (1) | JP2016516813A (pt) |
KR (1) | KR20160026856A (pt) |
CN (1) | CN105636966A (pt) |
AU (2) | AU2013386844A1 (pt) |
BR (1) | BR112015026362A2 (pt) |
CA (1) | CA2909597A1 (pt) |
MX (1) | MX2015014621A (pt) |
RU (1) | RU2015144372A (pt) |
WO (1) | WO2014171971A1 (pt) |
ZA (1) | ZA201508390B (pt) |
Families Citing this family (7)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2014026143A1 (en) * | 2012-08-09 | 2014-02-13 | Pono Corporation | Conjugated anti-microbial compounds and conjugated anti-cancer compounds and uses thereof |
US20160319322A1 (en) * | 2013-11-01 | 2016-11-03 | University Of Notre Dame Du Lac | Pathogen detection |
AU2015304860B2 (en) * | 2014-08-19 | 2020-07-16 | Hsiri Therapeutics, LLC | Antibacterial sideromycins |
US20210277023A1 (en) * | 2018-05-09 | 2021-09-09 | University Of Notre Dame Du Lac | Antibiotic conjugates |
WO2020263975A1 (en) * | 2019-06-24 | 2020-12-30 | Diverse Biotech, Inc. | Beta-lactam-cannabinoid conjugate molecules |
CN115557856B (zh) * | 2022-10-14 | 2024-03-19 | 福建省微生物研究所 | 一种嗜铁素类化合物Fradiamine C及其发酵菌株与发酵方法 |
CN118497240A (zh) * | 2023-05-04 | 2024-08-16 | 浙江大学 | 定向富集Ca.Brocadia的铁载体、突变株、制备方法及应用 |
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DE10111160A1 (de) | 2001-03-01 | 2002-09-05 | Gruenenthal Gmbh | Neue Catecholat-ß-Laktamkonjugate, Verfahren zu ihrer Herstellung und ihre Anwendung |
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2013
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- 2013-10-23 KR KR1020157032871A patent/KR20160026856A/ko not_active Application Discontinuation
- 2013-10-23 CN CN201380077567.2A patent/CN105636966A/zh active Pending
- 2013-10-23 RU RU2015144372A patent/RU2015144372A/ru not_active Application Discontinuation
- 2013-10-23 AU AU2013386844A patent/AU2013386844A1/en not_active Abandoned
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- 2013-10-23 BR BR112015026362A patent/BR112015026362A2/pt not_active IP Right Cessation
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2015
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ZA201508390B (en) | 2016-11-30 |
MX2015014621A (es) | 2016-09-07 |
US20130281424A1 (en) | 2013-10-24 |
AU2013386844A1 (en) | 2015-11-05 |
RU2015144372A (ru) | 2017-05-19 |
US9302012B2 (en) | 2016-04-05 |
EP2986617A1 (en) | 2016-02-24 |
KR20160026856A (ko) | 2016-03-09 |
WO2014171971A1 (en) | 2014-10-23 |
JP2016516813A (ja) | 2016-06-09 |
AU2018227936A1 (en) | 2018-09-27 |
CN105636966A (zh) | 2016-06-01 |
EP2986617A4 (en) | 2017-03-22 |
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