synthesis, antiplatelet activity and cytotoxicity assessment of indole-based hydrazone derivatives
نویسندگان
چکیده
a 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. based on the activity data, phenylhydrazone derivatives (1a-i) exhibited considerable antiplatelet activity and minimal toxic effect on platelet cells. the results of the present study could provide a better understanding of the structure activity relationship of antiplatelet indolehydrazones.
منابع مشابه
Synthesis, Antiplatelet Activity and Cytotoxicity Assessment of Indole-Based Hydrazone Derivatives
A 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 a...
متن کاملSynthesis, Antiplatelet Activity and Cytotoxicity Assessment of Indole-Based Hydrazone Derivatives
A 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 a...
متن کاملSynthesis, Antiplatelet Activity and Cytotoxicity Assessment of Indole-Based Hydrazone Derivatives
A 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 a...
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Melatonin (MLT) is a hormone synthesized from the pineal gland. It is a direct scavenger of free radicals, which is related to its capability to defend cells from oxidative stress. Recently MLT-related compounds are under investigation to establish which exhibit the maximum activity with the lowest side effects. In this study 5-chloroindole hydrazide/hydrazone derivatives were synthesized from ...
متن کاملAntimicrobial evaluation of indole-containing hydrazone derivatives.
There has been an increasing importance of drug-resistant pathogens in clinical microbiological and antibacterial research. Indoles and hydrazone-type compounds constitute important classes of compounds in the search for effective agents against multidrug-resistant microbial infections. In this study a series of 1-methylindole-3-carboxaldehyde hydrazone derivatives were evaluated for their in v...
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عنوان ژورنال:
iranian journal of pharmaceutical researchجلد ۱۴، شماره ۴، صفحات ۱۰۷۷-۱۰۸۶
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