Synthesis, Antiplatelet Activity and Cytotoxicity Assessment of Indole-Based Hydrazone Derivatives

AuthorKamaleddin Haj Mohammad Ebrahim Tehranien
AuthorMarjan Esfahani Zadehen
AuthorVida Mashayekhien
AuthorMaryam Hashemien
AuthorFarzad Kobarfarden
AuthorFarhad Gharebaghien
AuthorShohreh Mohebbien
Issued Date2015-10-31en
AbstractA series of indole-based aryl(aroyl)hydrazone analogs of antiplatelet indole-3-carboxaldehyde phenylhydrazone were synthesized by the Schiff base formation reaction and their antiplatelet activity was assessed using human platelet rich plasma. The platelet concentrate was obtained using a two-step centrifugation protocol and ADP, arachidonic acid and collagen were used as inducers of platelet aggregation. Based on the results, substituted phenylhydrazones showed promising activity. Among them, compound 1i was the most potent derivative with an IC50 comparable to that of indomethacin as a standard drug. The hydrazone derivatives were also tested for their cytotoxicity using on platelet concentrates and fibroblast L929 cells. The majority of the derivatives showed an acceptable selectivity towards antiplatelet aggregation activity.en
DOIhttps://doi.org/10.22037/ijpr.2015.1739en
KeywordIndoleen
KeywordArylhydrazoneen
KeywordAntiplatelet aggregationen
KeywordArachidonic aciden
KeywordCollagenen
PublisherBrieflandsen
TitleSynthesis, Antiplatelet Activity and Cytotoxicity Assessment of Indole-Based Hydrazone Derivativesen
TypeOriginal Articleen

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