Novel inhibitors of the methicillin-resistant Staphylococcus aureus (MRSA)-pyruvate kinase
Novel bisindolyl-cycloalkane indoles resulted from the reaction of aliphatic dialdehydes and indole. As bisindolyl-natural alkaloid compounds have recently been reported as inhibitors of the methicillin-resistant Staphylococcus aureus (MRSA)-pyruvate kinase (PK), we tested our novel compounds as MRS...
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| Veröffentlicht in: | Journal of enzyme inhibition and medicinal chemistry 2016-11, Vol.31 (6), p.1666-1671 |
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| container_end_page | 1671 |
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| container_issue | 6 |
| container_start_page | 1666 |
| container_title | Journal of enzyme inhibition and medicinal chemistry |
| container_volume | 31 |
| creator | El-Sayed, Mardia Telep Zoraghi, Roya Reiner, Neil Suzen, Sibel Ohlsen, Knut Lalk, Michael Altanlar, Nurten Hilgeroth, Andreas |
| description | Novel bisindolyl-cycloalkane indoles resulted from the reaction of aliphatic dialdehydes and indole. As bisindolyl-natural alkaloid compounds have recently been reported as inhibitors of the methicillin-resistant Staphylococcus aureus (MRSA)-pyruvate kinase (PK), we tested our novel compounds as MRSA PK inhibitors and now report first inhibiting activities. We discuss structure-activity relationships of structurally varied compounds. Activity influencing substituents have been characterized and relations to antibacterial activities of the most active compounds have been proved. |
| doi_str_mv | 10.3109/14756366.2015.1118685 |
| format | Article |
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As bisindolyl-natural alkaloid compounds have recently been reported as inhibitors of the methicillin-resistant Staphylococcus aureus (MRSA)-pyruvate kinase (PK), we tested our novel compounds as MRSA PK inhibitors and now report first inhibiting activities. We discuss structure-activity relationships of structurally varied compounds. 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| fulltext | fulltext |
| identifier | ISSN: 1475-6366 |
| ispartof | Journal of enzyme inhibition and medicinal chemistry, 2016-11, Vol.31 (6), p.1666-1671 |
| issn | 1475-6366 1475-6374 |
| language | eng |
| recordid | cdi_pubmed_primary_26653005 |
| source | MEDLINE; Free E-Journal (出版社公開部分のみ） |
| subjects | Anti-Bacterial Agents - pharmacology Antimicrobial compounds biological activity Enzyme Inhibitors - chemistry Enzyme Inhibitors - pharmacology indolyl-derived compounds Methicillin-Resistant Staphylococcus aureus - drug effects Methicillin-Resistant Staphylococcus aureus - enzymology Pyruvate Kinase - antagonists & inhibitors Spectrum Analysis - methods |
| title | Novel inhibitors of the methicillin-resistant Staphylococcus aureus (MRSA)-pyruvate kinase |
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