Synthesis and structure-activity relationships of novel abietane diterpenoids with activity against Staphylococcus aureus
Aim: To find alternative compounds against methicillin-resistant Staphylococcus aureus (MRSA) and methicillin-susceptible S. aureus (MSSA), novel derivatives from dehydroabietic acid were synthesized. Methods & results: Compound 12 was the most effective against 15 MRSA and 11 MSSA with minimum inhibitory concentration values ranging from 3.9 to 15.6 μg/ml. Although less active than 12, compound 11, followed by 25 and 13, also exhibited anti-staphylococcal activity. Additional studies showed that compound 12 is devoid of toxic effect on non-target cells. A structure-activity relationship study revealed that an oxime at C-13 together with a hydroxyl at C-12 could play a key role in the activity. Conclusion: These structures, in particular compound 12, could arise as templates for the development of agents against MRSA and MSSA.
| Medienart: |
E-Artikel |
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| Erscheinungsjahr: |
2019 |
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| Erschienen: |
2019 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:11 |
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| Enthalten in: |
Future medicinal chemistry - 11(2019), 24 vom: 21. Dez., Seite 3109-3124 |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Chabán, Macarena Funes [VerfasserIn] |
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| Links: |
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| Anmerkungen: |
Date Completed 10.07.2020 Date Revised 10.07.2020 published: Print Citation Status MEDLINE |
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| doi: |
10.4155/fmc-2019-0192 |
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| funding: |
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| Förderinstitution / Projekttitel: |
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| PPN (Katalog-ID): |
NLM304399663 |
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| 245 | 1 | 0 | |a Synthesis and structure-activity relationships of novel abietane diterpenoids with activity against Staphylococcus aureus |
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| 500 | |a Date Completed 10.07.2020 | ||
| 500 | |a Date Revised 10.07.2020 | ||
| 500 | |a published: Print | ||
| 500 | |a Citation Status MEDLINE | ||
| 520 | |a Aim: To find alternative compounds against methicillin-resistant Staphylococcus aureus (MRSA) and methicillin-susceptible S. aureus (MSSA), novel derivatives from dehydroabietic acid were synthesized. Methods & results: Compound 12 was the most effective against 15 MRSA and 11 MSSA with minimum inhibitory concentration values ranging from 3.9 to 15.6 μg/ml. Although less active than 12, compound 11, followed by 25 and 13, also exhibited anti-staphylococcal activity. Additional studies showed that compound 12 is devoid of toxic effect on non-target cells. A structure-activity relationship study revealed that an oxime at C-13 together with a hydroxyl at C-12 could play a key role in the activity. Conclusion: These structures, in particular compound 12, could arise as templates for the development of agents against MRSA and MSSA | ||
| 650 | 4 | |a Journal Article | |
| 650 | 4 | |a Research Support, Non-U.S. Gov't | |
| 650 | 4 | |a antibacterial activity | |
| 650 | 4 | |a dehydroabietic acid derivatives | |
| 650 | 4 | |a methicillin-resistant Staphylococcus aureus | |
| 650 | 4 | |a methicillin-susceptible Staphylococcus aureus | |
| 650 | 4 | |a structure−activity relationships | |
| 650 | 7 | |a Abietanes |2 NLM | |
| 650 | 7 | |a Anti-Bacterial Agents |2 NLM | |
| 700 | 1 | |a I Antoniou, Antonia |e verfasserin |4 aut | |
| 700 | 1 | |a Karagianni, Catherine |e verfasserin |4 aut | |
| 700 | 1 | |a Toumpa, Dimitra |e verfasserin |4 aut | |
| 700 | 1 | |a Joray, Mariana Belén |e verfasserin |4 aut | |
| 700 | 1 | |a Bocco, José Luis |e verfasserin |4 aut | |
| 700 | 1 | |a Sola, Claudia |e verfasserin |4 aut | |
| 700 | 1 | |a M Athanassopoulos, Constantinos |e verfasserin |4 aut | |
| 700 | 1 | |a Carpinella, María Cecilia |e verfasserin |4 aut | |
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