Por favor, use este identificador para citar o enlazar este ítem: https://hdl.handle.net/10495/11589
Título : Synthesis and Evaluation of Thiochroman-4-One Derivatives as Potential Leishmanicidal Agents
Autor : Vélez Bernal, Iván Darío
Robledo Restrepo, Sara María
Echeverri López, Luis Fernando
Quiñones Fletcher, Winston
metadata.dc.subject.*: Leishmania
Thiochroman-4-one
Thiochromones
Thioflavone
Vinyl sulfone
Fecha de publicación : 2017
Editorial : MDPI
Citación : Vargas E, Echeverri F, Vélez ID, Robledo SM, Quiñones W. Synthesis and Evaluation of Thiochroman-4-One Derivatives as Potential Leishmanicidal Agents. Molecules. 2017 Nov 29;22(12). pii: E2041
Resumen : ABSTARCT: The S-containing heterocyclic compounds benzothiopyrans or thiochromones stand out as having promising biological activities due to their structural relationship with chromones (benzopyrans), which are widely known as privileged scaffolds in medicinal chemistry. In this work, we report the synthesis of 35 thiochromone derivatives and the in vitro antileishmanial and cytotoxic activities. Compounds were tested against intracellular amastigotes of Leishmania panamensis and cytotoxic activity against human monocytes (U-937 ATCC CRL-1593.2). Compounds bearing a vinyl sulfone moiety, 4h, 4i, 4j, 4k, 4l and 4m, displayed the highest antileishmanial activity, with EC50 values lower than 10 μM and an index of selectivity over 100 for compounds 4j and 4l. When the double bond or the sulfone moiety was removed, the activity decreased. Our results show that thiochromones bearing a vinyl sulfone moiety are endowed with high antileishmanial activity and low cytotoxicity.
ISSN : 1420-3049
metadata.dc.identifier.doi: 10.3390/molecules22122041
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