6602-15-9Relevant academic research and scientific papers
Synthesis and evaluation of thiochroman-4-one derivatives as potential leishmanicidal agents
Vargas, Esteban,Echeverri, Fernando,Vélez, Iván D.,Robledo, Sara M.,Qui?ones, Wiston
, (2018/01/17)
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.
Benzodiazepine analogues. Part 8. Trimethylsilyl azide mediated Schmidt rearrangement of thioflavanone and thiochromanone precursors
Kaye,Mphahlele
, p. 1495 - 1509 (2007/10/02)
The synthesis and Schmidt rearrangement of a series of thioflavanone analogues to benzothiazepinone derivatives is described.
Chemotherapeutic agents
-
, (2008/06/13)
A method of treating or preventing viral infections, in particular rhinovirus infections comprising the administration of an effective amount of a 2-phenyltetralin derivative or a heterocyclic analogue thereof. Pharmaceutical compositions containing these compounds, and some novel compounds are also disclosed.
