776-88-5Relevant articles and documents
Evaluation of the Pharmacophoric Role of the O-O Bond in Synthetic Antileishmanial Compounds: Comparison between 1,2-Dioxanes and Tetrahydropyrans
Ortalli, Margherita,Varani, Stefania,Cimato, Giorgia,Veronesi, Ruben,Quintavalla, Arianna,Lombardo, Marco,Monari, Magda,Trombini, Claudio
, p. 13140 - 13158 (2020/11/13)
Leishmaniases are neglected diseases that can be treated with a limited drug arsenal; the development of new molecules is therefore a priority. Recent evidence indicates that endoperoxides, including artemisinin and its derivatives, possess antileishmanial activity. Here, 1,2-dioxanes were synthesized with their corresponding tetrahydropyrans lacking the peroxide bridge, to ascertain if this group is a key pharmacophoric requirement for the antileishmanial bioactivity. Newly synthesized compounds were examined in vitro, and their mechanism of action was preliminarily investigated. Three endoperoxides and their corresponding tetrahydropyrans effectively inhibited the growth of Leishmania donovani promastigotes and amastigotes, and iron did not play a significant role in their activation. Further, reactive oxygen species were produced in both endoperoxide-and tetrahydropyran-Treated promastigotes. In conclusion, the peroxide group proved not to be crucial for the antileishmanial bioactivity of endoperoxides, under the tested conditions. Our findings reveal the potential of both 1,2-dioxanes and tetrahydropyrans as lead compounds for novel therapies against Leishmania.
Phosphorus promoted SO42-/TiO2 solid acid catalyst for acetalization reaction
Zhong, Shaofeng,Ou, Qiongrong,Shao, Linjun
, p. 3005 - 3008 (2015/11/27)
A novel phosphorus modifed SO42-/TiO2 catalyst was synthesized by a facile coprecipitation method, followed by calcination. The catalytic performance of this novel solid acid was evaluated by acetalization. The results showed that the phosphorus was very effcient to enhance the catalytic activity of SO42-/TiO2. The solid acid owned high activity for the acetalization with the yields over 90%. Moreover, the solid acid could be reused for six times without loss of initial catalytic activities.
Four acid-catalysed dehydration reactions proceed without interference
Lirag, Rio Carlo,Miljani?, Ognjen ?.
supporting information, p. 9401 - 9404 (2014/08/05)
Four acid-catalysed dehydration reactions can proceed in one pot, simultaneously and without interference, to yield one imine, one acetal (or boronic ester), one ester and one alkene, even though many other cross-products could be conceived. This advanced