A5089763472- Crystallization and Solubility Studies
- Synthesis and Characterization of Heterocyclic Compounds
- X-ray Diffraction in Crystallography
- Asymmetric Synthesis and Catalysis
- Advanced Combustion Engine Technologies
- Chemical Synthesis and Analysis
- Chemical Synthesis and Reactions
- Catalytic Processes in Materials Science
- Synthesis and Reactions of Organic Compounds
- Asymmetric Hydrogenation and Catalysis
- Fuel Cells and Related Materials
- Biodiesel Production and Applications
- Synthetic Organic Chemistry Methods
- Synthesis and Biological Evaluation
- Cannabis and Cannabinoid Research
- Synthesis of heterocyclic compounds
- Industrial Engineering and Technologies
- Synthesis and Reactivity of Heterocycles
- Neuroscience and Neuropharmacology Research
- Axial and Atropisomeric Chirality Synthesis
- Neurotransmitter Receptor Influence on Behavior
- Geophysical Methods and Applications
- Electric and Hybrid Vehicle Technologies
- Catalytic Cross-Coupling Reactions
- Coordination Chemistry and Organometallics
University of Staffordshire
2019-2022
Loughborough University
2020
University of Bath
2006-2017
UNSW Sydney
2016
Evotec (United Kingdom)
2014-2015
GlaxoSmithKline (United Kingdom)
2002-2013
GlaxoSmithKline (China)
2011
Nuvera (Italy)
2006
Nuvera Biosciences (United States)
2005
University of Glasgow
2003
Selective CB2 receptor agonists are promising potential therapeutic agents for the treatment of inflammatory and neuropathic pain. A focused screen identified a pyrimidine ester as partial agonist at with micromolar potency. Subsequent lead optimization 35, GW842166X, optimal compound in series. 35 has an oral ED50 0.1 mg/kg rat FCA model pain was selected clinical candidate this indication.
The stable, readily available molybdenum(II) complexes [Mo(CO)(4)Br(2)](2) (B) and Mo(CO)(3)(MeCN)(2)(SnCl(3))Cl (C) have been found to catalyze C-C bond-forming allylic substitution with electron-rich aromatics (e.g., 15 + PhOMe --> 62) heteroaromatics 36 88) as nucleophiles under mild conditions (room temperature, 30 min-3 h). Remarkable is the para-selectivity for anisole, whereas phenol tends favor ortho-substitution in certain instances. Mechanistic stereochemical experiments are...
We report on the development of a series pyrimidine carboxylic acids that are potent and selective inhibitors kynurenine monooxygenase competitive for kynurenine. describe SAR this novel their inhibition KMO activity in biochemical cellular assays selectivity against other pathway enzymes. optimization process led to identification program lead compound with suitable ADME/PK profile therapeutic development. demonstrate systemic vivo provides pharmacodynamic evidence modulation metabolites...
During the normal dive, seal has a reflex bradycardia that is not accompanied by inversion of P waves or T atrial ventricular arrhythmias, although does have an occasional block conduction across A-V node during diving. The dive appears to be mediated through vagal stimulus. electrocardiograms voluntary diving and forced submersion with struggle are different.
We report the synthesis and SAR of a series novel azaindole CB(2) agonists. 6-Azaindole 18 showed activity in an acute pain model but was inactive chronic model. is Pgp substrate with low brain penetration. The template redesigned, resulting 5-azaindole 36 potent agonist high CNS This compound efficacious joint
The title binaphthyls 19 and 26, which are the positional isomers of 2-methoxy-2'-(diphenylphosphino)-1,1'-binaphthyl (MOP, 19) 2-amino-2'-hydroxy-1,1'-binaphthyl (NOBIN, 26), have been synthesized by Suzuki coupling as key step (10 + 15-->18), followed functional group transformations, involving C-P C-N bond formation (18-->19 18-->23). Racemic intermediate 22 was resolved co-crystallization with N-benzylcinchonidinium chloride absolute configuration determined X-ray crystallography. These...
An enantiopure amine tris(phenolate) ligand containing a single stereogenic center has been used to control the propeller-like chirality of derived pseudo-C3-symmetric titanium isopropoxide complex with excellent levels diastereocontrol.
A chiral pseudo-C3-symmetric titanium triflate that employs the point chirality of a single stereogenic centre to control propeller its aryl rings has been used catalyse an asymmetric sulfoxidation reaction.
The objective of personalization is to create a product that matches the exacting requirements individual consumer. Where these products must interface with changing dynamics human form, traditional manufacturing techniques, coupled paradigms do not enable efficient generation personalized products. Particularly when they encapsulate body-parts susceptible variations in dimension through daily activity. Emerging 3D printing methods are limited non-conforming rigid materials, wide tolerance...
Abstract Syntheses of 2‐amino‐7‐(2‐hydroxyethoxymethyl)imidazo[5,1‐ f ]‐1,2,4‐triazin‐4(3 H )‐one ( 2 ) and 6‐amino‐3‐(2‐hydroxyethoxymethyl)‐1,2,4‐triazolo[3,4‐ ]‐1,2,4‐triazin‐8(7 3 ), novel isosteres the antiviral agent acyclovir, are reported.
Arthur D. Little in conjunction with the Department of Energy and Illinois Commerce Community Affairs are developing an ethanol fuel processor for cell vehicles. Initial studies were carried out on a 25 kWe catalytic partial oxidation (POX) reformer to determine effect equivalence ratio, steam carbon residence time conversion. Results POX experiments show near equilibrium yields hydrogen monoxide ratio 3.0 efficiency 80%. The size weight prototype yield power densities 1.44 l/kW 1.74 kg/kW...
ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTCupration of Organomercurials: A Mild Method for the Intramolecular Addition Organometallics to Ester GroupsPavel Kocovsky, Jason M. Grech, and William L. MitchellCite this: J. Org. Chem. 1995, 60, 6, 1482–1483Publication Date (Print):March 1, 1995Publication History Published online1 May 2002Published inissue 1 March 1995https://pubs.acs.org/doi/10.1021/jo00111a002https://doi.org/10.1021/jo00111a002research-articleACS PublicationsRequest reuse...
ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTSynthesis and antiviral properties of 5-(2-substituted vinyl)-6-aza-2'-deoxyuridinesWilliam L. Mitchell, Paul Ravenscroft, Malcolm Hill, Lars J. S. Knutsen, Brian D. Judkins, Roger F. Newton, David I. C. ScopesCite this: Med. Chem. 1986, 29, 5, 809–816Publication Date (Print):May 1, 1986Publication History Published online1 May 2002Published inissue 1 1986https://doi.org/10.1021/jm00155a035RIGHTS & PERMISSIONSArticle...
As the market share of electric vehicles increases, intermittent load on electricity grid due to charging will increase. This can be counteracted by Vehicle-to-Grid (V2G) which utilises dormant feed power into grid, generating income for vehicle owner while relieving across grid. However, increased battery use through V2G negatively affect health. In this work, a computational model an with degradation is used investigate relationship these effects. The analysis was conducted at top level...
A short, efficient synthesis of novel imidazo-fused bridgehead-nitrogen C-nucleosides has been developed. Dehydrative coupling 2,5-anhydro-3,4,6-tri-O-benzoyl-D-allonic acid (14) with a series aminoalkyl-substituted heterocycles (6)–(8) gives the amides (15)–(17). The latter are subsequently converted into imidazo[1,5-a]pyridine, imidazo[1,5-a]pyrazine, imidazo[1,5-b]pyridazine, and imidazo[5,1-f]-1,2,4-triazine (20) (21). adenosine isostere, 8-amino-3-β-D-ribofuranosylimidazo[1,5-a]pyrazine...