Novel compounds of hybrid structure pyridazinone-coumarin as potent inhibitors of platelet aggregation
Aim: The current limitations of antiplatelet therapy promote the search for new antithrombotic agents. Here we describe novel platelet aggregation inhibitors that combine pyridazinone and coumarin scaffolds in their structure. Results: The target compounds were synthesized in good yield from maleic anhydride, following a multistep strategy. The in vitro studies demonstrated significant antiplatelet activity in many of these compounds, with IC50 values in the low micromolar range, revealing that the activity was affected by the substitution pattern of the two selected cores. Additional studies point out their effect as inhibitors of glycoprotein (Gp) IIb/IIIa activation. Conclusion: This novel hybrid structure can be considered a good prototype for the development of potent platelet aggregation inhibitors.
| 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), 16 vom: 17. Aug., Seite 2051-2062 |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Costas-Lago, María C [VerfasserIn] |
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| Links: |
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| Anmerkungen: |
Date Completed 22.06.2020 Date Revised 22.06.2020 published: Print Citation Status MEDLINE |
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| doi: |
10.4155/fmc-2018-0373 |
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| funding: |
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| Förderinstitution / Projekttitel: |
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| PPN (Katalog-ID): |
NLM30146541X |
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| 245 | 1 | 0 | |a Novel compounds of hybrid structure pyridazinone-coumarin as potent inhibitors of platelet aggregation |
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| 500 | |a Date Completed 22.06.2020 | ||
| 500 | |a Date Revised 22.06.2020 | ||
| 500 | |a published: Print | ||
| 500 | |a Citation Status MEDLINE | ||
| 520 | |a Aim: The current limitations of antiplatelet therapy promote the search for new antithrombotic agents. Here we describe novel platelet aggregation inhibitors that combine pyridazinone and coumarin scaffolds in their structure. Results: The target compounds were synthesized in good yield from maleic anhydride, following a multistep strategy. The in vitro studies demonstrated significant antiplatelet activity in many of these compounds, with IC50 values in the low micromolar range, revealing that the activity was affected by the substitution pattern of the two selected cores. Additional studies point out their effect as inhibitors of glycoprotein (Gp) IIb/IIIa activation. Conclusion: This novel hybrid structure can be considered a good prototype for the development of potent platelet aggregation inhibitors | ||
| 650 | 4 | |a Journal Article | |
| 650 | 4 | |a Research Support, Non-U.S. Gov't | |
| 650 | 4 | |a coumarin | |
| 650 | 4 | |a hybrid structures | |
| 650 | 4 | |a pharmacology | |
| 650 | 4 | |a platelet aggregation inhibitors | |
| 650 | 4 | |a pyridazinone | |
| 650 | 4 | |a synthetic chemistry | |
| 650 | 7 | |a Coumarins |2 NLM | |
| 650 | 7 | |a Platelet Aggregation Inhibitors |2 NLM | |
| 650 | 7 | |a Platelet Glycoprotein GPIIb-IIIa Complex |2 NLM | |
| 650 | 7 | |a Pyridazines |2 NLM | |
| 700 | 1 | |a Besada, Pedro |e verfasserin |4 aut | |
| 700 | 1 | |a Cano, Ernesto |e verfasserin |4 aut | |
| 700 | 1 | |a Terán, Carmen |e verfasserin |4 aut | |
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