All Outputs (25)

Characterisation of chlorinated, brominated and mixed halogenated dioxins, furans and biphenyls as potent and as partial agonists of the Aryl hydrocarbon receptor (2014)
Journal Article
Wall, R. J., Fernades, A., Rose, M., Bell, D. R., & Mellor, I. R. (2015). Characterisation of chlorinated, brominated and mixed halogenated dioxins, furans and biphenyls as potent and as partial agonists of the Aryl hydrocarbon receptor. Environment International, 76, 49-56. https://doi.org/10.1016/j.envint.2014.12.002

The Aryl hydrocarbon receptor (AhR) binds a variety of chlorinated and brominated dioxins, furans and biphenyls. Mixed halogenated variants have been recently identified in food at significant levels but full characterisation requires potency data in... Read More about Characterisation of chlorinated, brominated and mixed halogenated dioxins, furans and biphenyls as potent and as partial agonists of the Aryl hydrocarbon receptor.

The Effects of Conformational Constraints in the Polyamine Moiety of Philanthotoxins on AMPAR Inhibition (2014)
Journal Article
Franzyk, H., Grzeskowiak, J. W., Tikhonov, D. B., Jaroszewski, J. W., & Mellor, I. R. (2014). The Effects of Conformational Constraints in the Polyamine Moiety of Philanthotoxins on AMPAR Inhibition. ChemMedChem, 9(8), 1725-1731. https://doi.org/10.1002/cmdc.201402109

Philanthotoxin‐433 (PhTX‐433) is a known potent inhibitor of ionotropic glutamate receptors, and analogues have been synthesised to identify more potent and selective antagonists. Herein we report the synthesis of four PhTXs with a cyclopropane moiet... Read More about The Effects of Conformational Constraints in the Polyamine Moiety of Philanthotoxins on AMPAR Inhibition.

The antimalarial drug quinine interferes with serotonin biosynthesis and action (2014)
Journal Article
Islahudin, F., Tindall, S. M., Mellor, I. R., Swift, K., Christensen, H. E., Fone, K. C., …Avery, S. V. (2014). The antimalarial drug quinine interferes with serotonin biosynthesis and action. Scientific Reports, 4(3618), https://doi.org/10.1038/srep03618

The major antimalarial drug quinine perturbs uptake of the essential amino acid tryptophan, and patients with low plasma tryptophan are predisposed to adverse quinine reactions; symptoms of which are similar to indications of tryptophan depletion. As... Read More about The antimalarial drug quinine interferes with serotonin biosynthesis and action.

A two-directional approach to pyrrolizidines: total syntheses and biological evaluation of alkaloid cis-223B and (+/-)-xenovenine (2013)
Journal Article
Barthelme, A., Richards, D., Mellor, I. R., & Stockman, R. A. (2013). A two-directional approach to pyrrolizidines: total syntheses and biological evaluation of alkaloid cis-223B and (+/-)-xenovenine. Chemical Communications, 49(89), https://doi.org/10.1039/c3cc46800c

Total syntheses of alkaloid cis-223B and xenovenine are reported in 3 and 4 steps respectively using a two-directional synthesis/triple reductive amination strategy, and their neurotoxic properties assessed.

The bivalent ligand approach as a tool for improving the in vitro anti-alzheimer multitarget profile of dimebon (2013)
Journal Article
Rosini, M., Simoni, E., Bartolini, M., Soriano, E., Marco-Contelles, J., Andrisano, V., …Bolognesi, M. L. (2013). The bivalent ligand approach as a tool for improving the in vitro anti-alzheimer multitarget profile of dimebon. ChemMedChem, 8(8), 1276-1281. https://doi.org/10.1002/cmdc.201300263

Inspired by the concept of bivalent ligands, we prepared a small set of analogues of the drug candidate dimebon. They were shown to inhibit AChE, Aβ42 aggregation, and NMDA receptor activation to a greater extent than dimebon. Some of these compounds... Read More about The bivalent ligand approach as a tool for improving the in vitro anti-alzheimer multitarget profile of dimebon.