ORCID Profile
0000-0003-1642-1742
Current Organisations
The University of Edinburgh
,
University of York
,
Pharmaxis Ltd
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Publisher: Wiley
Date: 10-06-2017
DOI: 10.1111/BPH.13832
Publisher: Springer Science and Business Media LLC
Date: 20-03-2015
Publisher: American Chemical Society (ACS)
Date: 09-09-2005
DOI: 10.1021/AR050113T
Abstract: "One-pot" processes in which alcohol oxidations are combined with further elaboration of the carbonyl intermediate are reviewed. Sequential processes are briefly discussed, but most attention is centered on tandem processes that is, oxidations carried out in the presence of a nucleophilic trapping agent, rather than those in which the trapping agent is added after the oxidation is complete. As part of this Account, a comprehensive review of the discovery of tandem oxidation processes (TOP) will be given together with applications in alkene-forming reactions, cyclopropanations, and imine, oxime, amine, and heterocycle formation.
Publisher: American Chemical Society (ACS)
Date: 11-10-2003
DOI: 10.1021/OL035786V
Abstract: [reaction: see text] The first synthesis of the tetracyclic nucleus of the Integrastatins, natural products that have been shown to selectively inhibit HIV-1 integrase, is reported. Key steps of this synthesis involve a novel cis-selective Ramberg-Bäcklund reaction and an unusual Lewis acid-promoted cyclization step.
Publisher: Elsevier BV
Date: 06-2012
DOI: 10.1016/J.BMCL.2012.04.111
Abstract: A new class of 3-fluoroallyl amine-based SSAO/VAP-1 inhibitors is reported. These compounds have excellent selectivity over diamine oxidase, MAO-A and MAO-B. Synthesis and SAR studies leading to compound 28 (PXS-4159A) are reported. The pharmacokinetic profile of 28 in the rat, together with activity in a murine model of lung inflammation are also disclosed.
Publisher: Royal Society of Chemistry (RSC)
Date: 2009
DOI: 10.1039/B918860F
Abstract: Cross-linked hemoglobin-azides react with a bis-alkyne to form a bis-tetramer through sequential "click" reactions where the second step is promoted by the first.
Publisher: American Chemical Society (ACS)
Date: 11-06-2018
DOI: 10.1021/ACS.ORGLETT.8B01558
Abstract: The synthesis of the structure, 1, assigned to the anti-inflammatory natural product myrsinoic acid F is reported together with a means for preparing its Z-isomer 21. While neither of these compounds corresponds to the natural product, both of them are anti-inflammatory agents (as determined using a mouse ear edema assay) with congener 1 being notably more potent than the widely prescribed NSAID indometacin.
Publisher: American Chemical Society (ACS)
Date: 03-10-2019
DOI: 10.1021/ACS.JMEDCHEM.9B01283
Abstract: Lysyl oxidase-like 2 (LOXL2) is a secreted enzyme that catalyzes the formation of cross-links in extracellular matrix proteins, namely, collagen and elastin, and is indicated in fibrotic diseases. Herein, we report the identification and subsequent optimization of a series of indole-based fluoroallylamine inhibitors of LOXL2. The result of this medicinal chemistry c aign is
Publisher: Royal Society of Chemistry (RSC)
Date: 2004
DOI: 10.1039/B410786C
Publisher: Impact Journals, LLC
Date: 10-02-2017
Publisher: Royal Society of Chemistry (RSC)
Date: 2010
DOI: 10.1039/B922694J
Abstract: The need for an alternative to red cells for oxygen transport in transfusions has led to the creation of hemoglobin-based oxygen carriers, materials produced by chemical modification or genetic engineering of human or bovine hemoglobin. Modifications of the native proteins are necessitated by the spontaneous dissociation of the functional hemoglobin tetramers (alpha(2)beta(2)) into non-functional alphabeta dimers. Based on clinical observations of hypertension resulting from some of these materials, it was proposed that the stabilized tetramers are sufficiently small to extravasate through blood vessels and scavenge nitric oxide, depleting the endothelium of the signal for smooth muscle relaxation. In order to increase size and minimize extravasation while maintaining structure and function, methods for producing larger entities through protein-protein conjugation were developed. Approaches have included the use of nonspecific reagents that polymerize proteins (e.g., polyglutaraldehyde), conjugation to polyethylene glycol, expression of naturally occurring multimers and the use of selective reagents, which is the focus of this article.
Publisher: American Society for Pharmacology & Experimental Therapeutics (ASPET)
Date: 13-08-2013
Abstract: Semicarbazide-sensitive amine oxidase (SSAO), also known as vascular adhesion protein-1 (VAP-1), is a member of the copper-dependent amine oxidase family that is associated with various forms of inflammation and fibrosis. To investigate the therapeutic potential of SSAO/VAP-1 inhibition, potent and selective inhibitors with drug-like properties are required. PXS-4681A [(Z)-4-(2-(aminomethyl)-3-fluoroallyloxy)benzenesulfonamide hydrochloride] is a mechanism-based inhibitor of enzyme function with a pharmacokinetic and pharmacodynamic profile that ensures complete, long-lasting inhibition of the enzyme after a single low dose in vivo. PXS-4681A irreversibly inhibits the enzyme with an apparent Ki of 37 nM and a kinact of 0.26 min(-1) with no observed turnover in vitro. It is highly selective for SSAO/VAP-1 when profiled against related amine oxidases, ion channels, and seven-transmembrane domain receptors, and is superior to previously reported inhibitors. In mouse models of lung inflammation and localized inflammation, dosing of this molecule at 2 mg/kg attenuates neutrophil migration, tumor necrosis factor-α, and interleukin-6 levels. These results demonstrate the drug-like properties of PXS-4681A and its potential use in the treatment of inflammation.
Publisher: Wiley
Date: 11-2021
DOI: 10.1002/CTM2.572
Publisher: Royal Society of Chemistry (RSC)
Date: 2005
DOI: 10.1039/B418426B
Abstract: With certain substituent patterns, benzyl benzyl sulfone systems have been found to give unexpectedly high Z-stereoselectivity (up to E:Z = 1:16) in the Meyers variant of the Ramberg-Bäcklund reaction. A range of sulfones, bearing various aryl substituents, were explored to rationalize this unprecedented selectivity for Z-stilbene systems. This high level of double bond stereocontrol has also been utilized in the synthesis of integrastatin nucleus, the core of two highly bioactive anti-HIV compounds.
Publisher: Wiley
Date: 09-12-2018
DOI: 10.1111/JCMM.14074
Location: United Kingdom of Great Britain and Northern Ireland
Location: United Kingdom of Great Britain and Northern Ireland
No related grants have been discovered for Jonathan Foot.