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Amine–alkyl derivatives of hydantoin: New tool to combat resistant bacteria
- Source :
- European Journal of Medicinal Chemistry, European Journal of Medicinal Chemistry, Elsevier, 2011, 46 (12), pp.5807-5816. ⟨10.1016/j.ejmech.2011.09.032⟩
- Publication Year :
- 2011
- Publisher :
- Elsevier BV, 2011.
-
Abstract
- International audience; A series of new 5,5-diphenylhydantoin derivatives with various amineealkyl terminal fragments at N1-position were synthesized. Then a series of twenty-eight compounds with the same hydantoin scaffold were evaluated for their potency to combat bacterial MultiDrug Resistance (MDR). Intrinsic antibacterial activities were first evaluated. As these compounds showed no direct activity on bacteria, their influence on minimal inhibitory concentration (MIC) of nalidixic acid was tested in two strains of Enterobacter aerogenes: the reference-strain ATCC-13048 and the CM-64 strain which over-produces AcrAB-TolC efflux pump. The compounds showed moderate-or low-anti-MDR properties. According to SAR-studies, hit compounds containing 2-methoxyphenylpiperazine at N1-terminal fragment and methylcarboxyl acid one at N3-position of hydantoin have been identified for further microbiological studies and pharma-comodulations to develop efflux pump inhibitors.
- Subjects :
- antibiotic resistance
Nalidixic acid
Antibiotic resistance
Stereochemistry
[CHIM.THER] Chemical Sciences/Medicinal Chemistry
efflux pumps
Hydantoin
Microbial Sensitivity Tests
[CHIM.THER]Chemical Sciences/Medicinal Chemistry
010402 general chemistry
Enterobacter aerogenes
01 natural sciences
Nalidixic Acid
Structure-Activity Relationship
chemistry.chemical_compound
Minimum inhibitory concentration
Bacterial Proteins
Drug Resistance, Multiple, Bacterial
Drug Discovery
medicine
Humans
Efflux pumps
Amines
Pharmacology
biology
010405 organic chemistry
Chemistry
Hydantoins
Organic Chemistry
Enterobacteriaceae Infections
General Medicine
biology.organism_classification
Hydantoin derivatives
Anti-Bacterial Agents
hydantoin derivatives
0104 chemical sciences
3. Good health
Multiple drug resistance
chemosensitizer
Chemosensitizer
Amine gas treating
Efflux
Carrier Proteins
Bacteria
medicine.drug
Subjects
Details
- ISSN :
- 02235234 and 17683254
- Volume :
- 46
- Database :
- OpenAIRE
- Journal :
- European Journal of Medicinal Chemistry
- Accession number :
- edsair.doi.dedup.....90d22b856e59e0a9d62f2e5fb1bc1425