Synthesis of 4-Methoxy-1, 3-Benzenediolylhydrazones and Evaluation of Their Anti-Platelet Aggregation Activity

AuthorChaoqing Wangen
AuthorYan Wangen
AuthorQingsong Dengen
AuthorXiujie Liuen
Issued Date2019-10-31en
AbstractIn our present investigation, a series of novel 4-methoxy-1,3-benzenediolyl-hydrazones were designed and synthesized, and their ability to inhibit platelet aggregation was evaluated by adenosine diphosphate (ADP) and arachidonic acid (AA). The structures of the synthesized compounds were confirmed by spectral data. Results demonstrated that the activities of all compounds excelled the positive drug Picotamide (25.1% inhibition rate) and seven compounds (PNN01, PNN03, PNN05, PNN07, PNN09, PNN12, and PNN14) have efficiently inhibited platelet aggregation even higher than Clopidogrel (37.6% inhibition rate) induced by AA. Among them, PNN07 (39.8% inhibition rate) was considered as the most potent analogue. Evaluation of cytotoxic activity of the compounds against L929 cell line revealed that none of the compounds have significant cytotoxicity. Thus, diolylhydrazones derives are potential to be antiplatelet aggregation inhibitors and maybe working in AA-induced selectively.en
DOIhttps://doi.org/10.22037/ijpr.2019.1100856en
Keyword4-Methoxy-1en
Keyword3-benzenediolylhydrazonesen
KeywordAnti-platelet aggregationen
KeywordCytotoxicityen
KeywordPicotamideen
PublisherBrieflandsen
TitleSynthesis of 4-Methoxy-1, 3-Benzenediolylhydrazones and Evaluation of Their Anti-Platelet Aggregation Activityen
TypeOriginal Articleen

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