Design, Synthesis, Structure‐Activity Relationship and Docking Studies of Novel Functionalized Arylvinyl‐1,2,4‐Trioxanes as Potent Antiplasmodial as well as Anticancer Agents
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DOI: 10.1002/cmdc.202000045
Abstract: A novel series of synthetic functionalized arylvinyl‐1,2,4‐trioxanes (8 a–p) has been prepared and assessed for their in vitro antiplasmodial activity against the chloroquine‐resistant Pf INDO strain of Plasmodium falciparum by using a SYBR green‐I fluorescence assay. Compounds… read more here.
Keywords: functionalized arylvinyl; docking studies; arylvinyl trioxanes; ic50 ... See more keywords
Novel halogenated arylvinyl-1,2,4 trioxanes as potent antiplasmodial as well as anticancer agents: Synthesis, bioevaluation, structure-activity relationship and in-silico studies.
Sign Up to like & getrecommendations! Published in 2021 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2021.113685
Abstract: Herein, we have synthesized a series of lipophilic, halogenated-arylvinyl-1,2,4-trioxanes 8a-g (28 compounds) and assessed for their in vitro anti-plasmodial activity in Plasmodium falciparum culture using SYBRgreen-I fluorescence assay against chloroquine-resistant Pf INDO and artemisinin-resistant Pf Cam… read more here.
Keywords: cell; halogenated arylvinyl; arylvinyl trioxanes; ic50 ... See more keywords
Reduction of the Double Bond of 6-Arylvinyl-1,2,4-trioxanes Leads to a Remarkable Increase in Their Antimalarial Activity against Multidrug-Resistant Plasmodium yoelii nigeriensis in a Swiss Mice Model
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DOI: 10.1021/acsomega.1c05041
Abstract: Novel 6-arylethyl-1,2,4-trioxanes6a–i and 7a–i are easily accessible in one step from the diimide reduction of 6-arylvinyl-1,2,4-trioxanes 5a–i. All of these new trioxanes were assessed for their oral antimalarial activity against multidrug-resistant Plasmodium yoelii nigeriensis in… read more here.
Keywords: protection; arylvinyl trioxanes; antimalarial activity; dose days ... See more keywords
Mechanistic Evaluation of the Stability of Arylvinyl-1,2,4-trioxanes under Acidic Conditions for Their Oral Administration as an Antimalarial Drug
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DOI: 10.1021/acsomega.2c01321
Abstract: A mechanistic approach to understand the course of metabolism for synthetic 1,2,4-trioxanes, potent antimalarial compounds, to evaluate their bioavailability for antimalarial action has been studied in the present work. It is an important parameter to… read more here.
Keywords: stability arylvinyl; mechanistic evaluation; arylvinyl trioxanes; drug ... See more keywords