All Outputs (8)

Lead optimisation of dehydroemetine for repositioned use in malaria (2020)
Journal Article
Panwar, P., Burusco, K., Abubaker, M., Matthews, H., Gutnov, A., Fernández-Álvaro, E., …Nirmalan, N. (2020). Lead optimisation of dehydroemetine for repositioned use in malaria. Antimicrobial Agents and Chemotherapy, 64(4), 1-10. https://doi.org/10.1128/AAC.01444-19

Drug repositioning offers an effective alternative to de novo drug design to tackle the urgent need for novel anti-malarial treatments. The anti-amoebic compound, emetine dihydrochloride, has been identified as a potent in-vitro inhibitor of the mult... Read More about Lead optimisation of dehydroemetine for repositioned use in malaria.

A novel role for small molecule glycomimetics in the protection against lipid-induced endothelial dysfunction : Involvement of Akt/eNOS and Nrf2/ARE signaling (2016)
Journal Article
Mahmoud, A., Wilkinson, F., Jones, A., Wilkinson, J., Romero, M., Duarte, J., & Alexander, M. (2017). A novel role for small molecule glycomimetics in the protection against lipid-induced endothelial dysfunction : Involvement of Akt/eNOS and Nrf2/ARE signaling. BBA - General Subjects, 1861(1.A), 3311-3322. https://doi.org/10.1016/j.bbagen.2016.08.013

Background: Glycomimetics are a diverse array of saccharide-inspired compounds, designed to mimic the bioactive functions of glycosaminoglycans. Therefore, glycomimetics represent a unique source of novel therapies to target aberrant signaling and... Read More about A novel role for small molecule glycomimetics in the protection against lipid-induced endothelial dysfunction : Involvement of Akt/eNOS and Nrf2/ARE signaling.

Expanding the scope of the Babler-Daubin oxidation : 1,3-oxidative transposition of secondary allylic alcohols (2016)
Journal Article
Killoran, P., Rossington, S., Wilkinson, J., & Hadfield, J. (2016). Expanding the scope of the Babler-Daubin oxidation : 1,3-oxidative transposition of secondary allylic alcohols. Tetrahedron Letters, 57(35), 3954-3957. https://doi.org/10.1016/j.tetlet.2016.07.076

We report the catalytic chromium-mediated oxidation of secondary allylic alcohols to give α,β-unsaturated aldehydes with exclusive (E)-stereoselectivity. This facile procedure employs catalytic PCC (5 mol%) and periodic acid (H5IO6) as a co-oxidant.... Read More about Expanding the scope of the Babler-Daubin oxidation : 1,3-oxidative transposition of secondary allylic alcohols.

Asymmetric synthesis of diarylmethane derivatives by dynamic kinetic resolution (2015)
Journal Article
kinetic resolution. Tetrahedron Letters, 56(26), 4025-4027. https://doi.org/10.1016/j.tetlet.2015.05.006

Asymmetric allylation of ortho-methoxydiphenylmethane has been carried out with high yields and ee of up to 94% using the chiral ligand (−)-sparteine as an additive. Results of reactions performed under various conditions suggest that a dynamic kinet... Read More about Asymmetric synthesis of diarylmethane derivatives by dynamic kinetic resolution.

Asymmetric alkylation of diarylmethane derivatives (2006)
Journal Article
Wilkinson, J., Rossington, S., Ducki, S., Leonard, J., & Hussain, N. (2006). Asymmetric alkylation of diarylmethane derivatives. Tetrahedron, 62(8), 1833-1844. https://doi.org/10.1016/j.tet.2005.11.044

Deprotonation–alkylation of prochiral diarylmethane substrates using sec-BuLi and (−)-sparteine has been carried out in excellent yields and up to 94% ee. A variety of enantioselective alkylations, silylations and stannylations have been performed on... Read More about Asymmetric alkylation of diarylmethane derivatives.

Towards the total synthesis of tangutorine by intramolecular Diels–Alder reaction (2005)
Journal Article
Wilkinson, J., Ardes-Guisot, N., Ducki, S., & Leonard, J. (2005). Towards the total synthesis of tangutorine by intramolecular Diels–Alder reaction. Tetrahedron Letters, 46(46), 8053-8056. https://doi.org/10.1016/j.tetlet.2005.09.058

The syntheses of 3,5-disubstituted-2-sulfolenes, and their participation in Pictet-Spengler reactions to give precursors of tangutorine, are described.

Asymmetric alkylation of diarylmethane derivatives. Improved results using methoxyethoxy substituent (2004)
Journal Article
Wilkinson, J., Rossington, S., Leonard, J., & Hussain, N. (2004). Asymmetric alkylation of diarylmethane derivatives. Improved results using methoxyethoxy substituent. Tetrahedron Letters, 45(28), 5481-5483. https://doi.org/10.1016/j.tetlet.2004.05.058

Alkylation of 2-methoxyethoxyphenyl phenyl methane using sec-BuLi and (−)-sparteine has been carried out in excellent yields and up to 94% ee. The best results were obtained in allylation reactions but methylation, ethylation, benzylation and trimeth... Read More about Asymmetric alkylation of diarylmethane derivatives. Improved results using methoxyethoxy substituent.

Asymmetric alkylation of diphenylmethane derivatives using (-)-sparteine (2004)
Journal Article
Wilkinson, J., Rossington, S., Leonard, J., & Hussain, N. (2004). Asymmetric alkylation of diphenylmethane derivatives using (-)-sparteine. Tetrahedron Letters, 45(6), 1191-1193. https://doi.org/10.1016/j.tetlet.2003.11.138

Alkylation of 2-oxygenated diphenylmethane derivatives using sec-butyllithium and (−)-sparteine gave enantiomeric excesses of up to 60% with allyl bromide but alkylations with methyl electrophiles were poorly selective. When compounds with a free hyd... Read More about Asymmetric alkylation of diphenylmethane derivatives using (-)-sparteine.