A5001071662- Carbohydrate Chemistry and Synthesis
- X-ray Diffraction in Crystallography
- Crystallization and Solubility Studies
- Chemical Synthesis and Analysis
- Glycosylation and Glycoproteins Research
- Diet, Metabolism, and Disease
- Enzyme Structure and Function
- Biochemical and Molecular Research
- Crystal structures of chemical compounds
- Organoboron and organosilicon chemistry
- Click Chemistry and Applications
- Heart Failure Treatment and Management
- Asymmetric Hydrogenation and Catalysis
- Signaling Pathways in Disease
- Enzyme Catalysis and Immobilization
- Nanomaterials for catalytic reactions
- Boron Compounds in Chemistry
- Fluorine in Organic Chemistry
- Innovative Microfluidic and Catalytic Techniques Innovation
- Organometallic Compounds Synthesis and Characterization
- Microbial Natural Products and Biosynthesis
- Analytical Chemistry and Chromatography
- Metal complexes synthesis and properties
- Cancer, Hypoxia, and Metabolism
- Computational Drug Discovery Methods
University of Newcastle Australia
2016-2025
Commonwealth Scientific and Industrial Research Organisation
2023-2025
Mitsubishi Tanabe Pharma Corporation
2023-2024
University of Bonn
2022
Callaghan Innovation
2015-2019
The University of Sydney
2011-2016
University College London
2011-2015
University of Oxford
2004-2012
Mansfield University
2004-2012
Wolfson Foundation
2011
The endothelium plays a fundamental role in maintaining vascular homeostasis by releasing factors that regulate local blood flow, systemic pressure, and the reactivity of leukocytes platelets. Accordingly, endothelial dysfunction underpins many cardiovascular diseases, including hypertension, myocardial infarction, stroke. Herein, we evaluated mice with endothelial-specific deletion Nppc, which encodes C-type natriuretic peptide (CNP), determined this mediator is essential for multiple...
The mitochondrial permeability transition pore is a recognized drug target for neurodegenerative conditions such as multiple sclerosis and ischemia-reperfusion injury in the brain heart. peptidylprolyl isomerase, cyclophilin D (CypD, PPIF), positive regulator of pore, genetic down-regulation or knock-out improves outcomes disease models. Current inhibitors isomerases show no selectivity between tightly conserved paralogs exhibit significant off-target effects, immunosuppression, toxicity. We...
This paper describes the first detailed NMR analysis of borylated intermediates and target compounds for a small library pyrrolidine iminosugars l-gulose absolute stereochemical configuration. The were functionalised via N-alkylation to bear boronate ester or boronic acid groups. addition organic boron pharmacophore allows further explore chemical space around in active sites, where atom has capability make reversible covalent bonds with enzyme nucleophiles other nucleophiles. We discuss...
Six new organotin(IV) compounds of Schiff bases derived from S-R-dithiocarbazate [R = benzyl (B), 2- or 4-methylbenzyl (2M and 4M, respectively)] condensed with 2-hydroxy-3-methoxybenzaldehyde (oVa) were synthesised characterised by elemental analysis, various spectroscopic techniques including infrared, UV-vis, multinuclear (1H, 13C, 119Sn) NMR mass spectrometry, single crystal X-ray diffraction. The the reaction Ph2SnCl2 Me2SnCl2 (S2MoVaH/S4MoVaH/SBoVaH) to form a total six that had...
Ionic liquids (ILs) have advantageous physical properties, which resulted in a rapid growth of research this area the past 15 years. One biggest challenges preventing widespread use ILs is cost production due to complex synthetic routes and/or expensive starting materials. Keeping mind these industrial needs for scale-up and desirable properties applications lubrification area, here, we report design synthesis four novel series hydrophobic room-temperature (RTILs) achieved from cheap...
Mitochondrial CyP-D (cyclophilin-D) catalyses formation of the PT (permeability transition) pore, a key lesion in pathogenesis I/R (ischaemia/reperfusion) injury. There is evidence [Malouitre, Dube, Selwood and Crompton (2010) Biochem. J. 425, 137-148] that cytoprotection by CyP inhibitor CsA (cyclosporin A) improved selective targeting to mitochondria. To investigate this further, we have developed an mtCsA (mitochondrial-targeted CsA) modifying spacer linking TPP+ (triphenylphosphonium)...
A novel series of 8-amino imidazo[1,2-a]pyrazine derivatives has been developed as inhibitors the VirB11 ATPase HP0525, a key component bacterial type IV secretion system. flexible synthetic route to both 2- and 3-aryl substituted regioisomers developed. The resulting imidazo[1,2-a]pyrazines used probe structure–activity relationships these inhibitors, which show potential antibacterial agents.
Cystic fibrosis (CF) is a debilitating disease caused by mutations in the cystic transmembrane conductance regulator (CFTR) gene, which codes for Cl-/HCO3 - channel. F508del, most common CF-associated mutation, causes both gating and biogenesis defects CFTR protein. This paper describes optimization of two fluorescence assays, capable measuring function cellular localization, their use pilot drug screen.HEK293 cells expressing YFP-F508del-CFTR, halide sensitive YFP tagged to N-terminal CFTR,...
Infrared ion-dip spectroscopy coupled with DFT and ab initio calculations are used to establish the intrinsic conformational preference of basic structural unit a peptide mimic, cis-tetrahydrofuran-based "carbopeptoid" (amide−sugar−amide), isolated at low temperature in gas phase. The carbopeptoid units form β-turn-type structure, stabilized by an intramolecular NH → OC hydrogen bond across sugar ring, thus forming 10-membered, C10 turn. Despite clear for β-turn structures unit, however,...
A commonly observed limitation of conducting hydrogenations under flow chemistry conditions is hydrodehalogenation.
Abstract Three homochiral polyhydroxylated piperidines containing a quaternary carbon branch at C‐2 of the heterocyclic ring, which can be considered as branched analogues deoxymannorijimycin (DMJ), and their corresponding lactams were synthesised from readily available versatile carbohydrate lactones 2‐ C ‐hydroxymethyl branch. The key step in synthesis these iminosugars, 1,5‐dideoxy‐2‐ ‐hydroxymethyl‐1,5‐imino‐ D ‐mannitol, L ‐gulitol ‐talitol, was an efficient modified Kiliani reaction...