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Stilbene-pyridazinone hybrids: design, synthesis and in vitro antiplatelet activity screening
[Display omitted] •Eighteen stilbene-pyridazinone hybrids were designed and synthesized.•The synthesis was performed from simple starting materials by using Wittig’s reaction.•The target compounds were studied in vitro as platelet aggregation inhibitors.•Most of the target compounds displayed better...
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Published in: | Bioorganic chemistry 2024-09, Vol.150, p.107615, Article 107615 |
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Main Authors: | , , , , |
Format: | Article |
Language: | English |
Subjects: | |
Citations: | Items that this one cites |
Online Access: | Get full text |
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Summary: | [Display omitted]
•Eighteen stilbene-pyridazinone hybrids were designed and synthesized.•The synthesis was performed from simple starting materials by using Wittig’s reaction.•The target compounds were studied in vitro as platelet aggregation inhibitors.•Most of the target compounds displayed better in vitro activity than resveratrol.•Pharmacokinetic and toxicity predictions point-out good drug-like properties.
A series of stilbene analogues, in which a phenyl ring was replaced by the pyridazin-3(2H)-one nucleus, was designed and synthesized to be explored as platelet aggregation inhibitors. The proposed stilbene-pyridazinone hybrids were successfully obtained from simple starting materials and by Wittig’s reaction. Most of the target compounds displayed improved in vitro activity in comparison with the standard drug, resveratrol, highlighting as the most potent the analogues 10d and 10e, with inhibition percentages of 94.15 % at 100 µM and 100 % at 50 µM, respectively.
The pharmacokinetic and toxicity (ADME/T) properties of the novel hybrids were also estimated with the SwissADME and ProTox-II web servers. |
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ISSN: | 0045-2068 1090-2120 1090-2120 |
DOI: | 10.1016/j.bioorg.2024.107615 |