Synthesis and biological activity of O56-substituted carboxyesters and carboxamides of teicoplanin aglycone
Autor: | Romeo Ciabatti, Pierfausto Seneci, Roberto Scotti, Aldo Trani, Pietro Ferrari |
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Rok vydání: | 1992 |
Předmět: |
Pharmacology
Steric effects Magnetic Resonance Spectroscopy Stereochemistry Chemistry medicine.drug_class Ionic bonding Biological activity Carboxamide Microbial Sensitivity Tests Gram-Positive Bacteria Antimicrobial Chemical synthesis Anti-Bacterial Agents Structure-Activity Relationship Gram-Negative Bacteria Drug Discovery medicine Molecule Teicoplanin Antibacterial agent |
Zdroj: | Scopus-Elsevier |
ISSN: | 1881-1469 0021-8820 |
DOI: | 10.7164/antibiotics.45.1633 |
Popis: | A series of O56-substituted carboxyester or carboxyamide derivatives of deglucoteicoplanin (TD) was prepared by condensation of the 56-hydroxyl function with various alkylating agents of general formula RBr, where R represents functional groups with different physico-chemical properties. The modifications at position 56 influenced the antimicrobial activity of the new derivatives; activity depended on the structure of various R groups, their ionic properties, and their steric hindrance. The activity of the new compounds did not show any significant improvement when compared with TD. The physico-chemical and antibacterial properties of the synthesized compounds are reported. |
Databáze: | OpenAIRE |
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