22337-78-6Relevant articles and documents
Structure-Based Design, Synthesis and Biological Evaluation of Bis-Tetrahydropyran Furan Acetogenin Mimics Targeting the Trypanosomatid F1 Component of ATP Synthase
Zacharova, Marija K.,Tulloch, Lindsay B.,Gould, Eoin R.,Fraser, Andrew L.,King, Elizabeth F.,Menzies, Stefanie K.,Smith, Terry K.,Florence, Gordon J.
, p. 5434 - 5440 (2019)
The protozoan parasites Trypanosoma brucei, Trypanosoma cruzi and Leishmania spp. are responsible for the severely debilitating neglected Tropical diseases of African sleeping sickness, Chagas disease and leishmaniasis, respectively. As part of our ongoing programme exploring the potential of simplified analogues of the acetogenin chamuvarinin we identified the T. brucei FoF1-ATP synthase as a target of our earlier triazole analogue series. Using computational docking studies, we hypothesised that the central triazole heterocyclic spacer could be substituted for a central 2,5-substituted furan moiety, thus diversifying the chemical framework for the generation of compounds with greater potency and/or selectivity. Here we report the design, docking, synthesis and biological evaluation of new series of trypanocidal compounds and demonstrate their on-target inhibitory effects. Furthermore, the synthesis of furans by the modular coupling of alkyne- and aldehyde-THPs to bis-THP 1,4-alkyne diols followed by ruthenium/xantphos-catalysed heterocyclisation described here represents the most complex use of this method of heterocyclisation to date.
Insight into the mechanism of decarbonylation of methanol by ruthenium complexes; a deuterium labelling study
Lorusso, Patrizia,Eastham, Graham R.,Cole-Hamilton, David J.
, p. 9411 - 9417 (2018)
In the reaction of [RuHClP3] (P = PPh3) with NaOMe in methanol, the product is [RuH2(CO)P3]. Short reaction times show that the final product is formed through [RuH4P3] as the major interme
A new oxidative addition of ruthenium(O) into an aryl halide bond and subsequent intermolecular C-H insertion
Grounds, Helen,Anderson, James C.,Hayter, Barry,Blake, Alexander J.
, p. 5289 - 5292 (2010/01/29)
Summary: An unprecedented oxidative insertion of the activated ruthenium complex Quot;Ru(CO)(PPh3)2" into aryl halide bonds enables a novel preparation of stable five-coordinate 16-electron d(6) o-aryl-Ru(II) complex Ru(CO)(p-C6
