Identification of 3-Phenylaminoquinolinium and 3-Phenylaminopyridinium salts as New Agents against Opportunistic Fungal Pathogens
Autor: | Jagan R. Etukala, Larry A. Walker, Shabana I. Khan, Seth Y. Ablordeppey, Tryphon Mazu, Melissa R. Jacob, Xue Y. Zhu |
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Jazyk: | angličtina |
Rok vydání: | 2010 |
Předmět: |
Antifungal Agents
Magnetic Resonance Spectroscopy Pyridines Clinical Biochemistry Pharmaceutical Science macromolecular substances Microbial Sensitivity Tests Biochemistry Article Aspergillus fumigatus chemistry.chemical_compound Structure-Activity Relationship Drug Discovery Candida albicans Structure–activity relationship Potency Cytotoxicity Molecular Biology Antibacterial agent biology Chemistry Alkaloid Organic Chemistry biology.organism_classification Cryptolepine Cyclization Cryptococcus neoformans Quinolines Molecular Medicine |
Popis: | Previous studies on the indoloquinoline alkaloid, cryptolepine (2), revealed that it has antii-nfective properties among other activities. Using Structure-activity relationship (SAR) techniques, several ring-opened analogs of cryptolepine (3-phenylaminopyridinium and 3-phenylaminoquinolinium derivatives) were designed to improve the potency and lower the cytotoxicity shown by several of the precursor agents. Results indicate that these ring-opened analogs constitute new anti-infective agents with over a 100-fold potency and several fold lower cytotoxicity than cryptolepine from which they are derived. |
Databáze: | OpenAIRE |
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