A5039195359- Crystallization and Solubility Studies
- X-ray Diffraction in Crystallography
- Cannabis and Cannabinoid Research
- Analytical Chemistry and Chromatography
- Neurotransmitter Receptor Influence on Behavior
- Pharmacological Receptor Mechanisms and Effects
- Forensic Toxicology and Drug Analysis
- Ion Channels and Receptors
- Protein purification and stability
- Biochemical Analysis and Sensing Techniques
- Microfluidic and Capillary Electrophoresis Applications
- Biochemical and Molecular Research
- Marine Biology and Environmental Chemistry
- Crystallography and molecular interactions
- Trypanosoma species research and implications
- Bioactive Compounds and Antitumor Agents
- Surface Modification and Superhydrophobicity
- Research on Leishmaniasis Studies
- HIV/AIDS drug development and treatment
- Silicone and Siloxane Chemistry
- Biosimilars and Bioanalytical Methods
- Tuberculosis Research and Epidemiology
- Cholesterol and Lipid Metabolism
- Peroxisome Proliferator-Activated Receptors
- Parasitic Infections and Diagnostics
University of Dundee
2018-2025
Wellcome Centre for Anti-Infectives Research
2020-2022
University of Strathclyde
2010-2018
Engineering and Physical Sciences Research Council
2017
Merck & Co., Inc., Rahway, NJ, USA (United States)
2011
Merck (United Kingdom)
2011
NHS Lanarkshire
2010-2011
University of Portsmouth
1994-1997
Early warning systems detect new psychoactive substances (NPS), while dedicated monitoring programs and routine drug toxicology testing identify fluctuations in prevalence. We report the increasing prevalence of synthetic cannabinoid receptor agonist (SCRA) ADB-BUTINACA (N-[1-amino-3,3-dimethyl-1-oxobutan-2-yl]-1-butyl-1H-indazole-3-carbox-amide). was first detected a seizure Sweden 2019, we its detection 13 Swedish forensic cases soon after. In January 2021, SCRA-infused papers seized...
There is an urgent need for new treatments Chagas disease, a parasitic infection which mostly impacts South and Central America. We previously reported on the discovery of GSK3494245/DDD01305143, preclinical candidate visceral leishmaniasis acted through inhibition Leishmania proteasome. A related analogue, active against Trypanosoma cruzi, showed suboptimal efficacy in animal model so alternative proteasome inhibitors were investigated. Screening library phenotypically analogues T. cruzi...
Although not currently in the infectious disease spotlight, there is still a pressing need for new agents to treat tuberculosis caused by Mycobacterium tuberculosis. As an ever-increasing amount of clinical resistance current drugs, ideally drugs would be found against novel targets circumvent pre-existing resistance. A phenotypic growth screen identified singleton, 1, as inhibitor M. growth. Mechanism-of-action studies determined that 1 targeted Pks13, essential enzyme cell wall...
Artemisinin-based combination therapies have been crucial in driving down the global burden of malaria, world's largest parasitic killer. However, their efficacy is now threatened by emergence resistance Southeast Asia and sub-Saharan Africa. Thus, there a pressing need to develop new antimalarials with diverse mechanisms action. One area Plasmodium metabolism that has recently proven rich exploitable antimalarial targets protein synthesis, compound targeting elongation factor 2 clinical...
Livestock diseases caused by Trypanosoma congolense , T . vivax and brucei collectively known as nagana, are responsible for billions of dollars in lost food production annually. There is an urgent need novel therapeutics. Encouragingly, promising antitrypanosomal benzoxaboroles under veterinary development. Here, we show that the most efficacious subclass these compounds prodrugs activated trypanosome serine carboxypeptidases (CBPs). Drug-resistance to a development candidate, AN11736,...
A novel CB1 receptor agonist lead series was identified using a high-throughput screening approach. The initial screen afforded single confirmed hit with poor water solubility. Structural variations were explored the aim of introducing solubility and improving potency. This led to discovery Org 28611, potent, soluble agonist, which selected for clinical evaluation as potential intravenous analgesic agent.
The performances of some silicone elastomers as compliant coatings which are resistant to marine fouling have been assessed from a sea-water exposure trial covering three seasons. Measurements contact angles (polar and non-polar liquids, recently-advanced recently-receded liquid drops air bubbles) used investigate the surface properties materials after two years' exposure. unmodified poly (dimethyIsiloxane) elastomer General Electric (GE) 21 was still settlement seasons...
A data set consisting of structures and aqueous solubility melting point for 51 salt forms the phenylethylamine base methylephedrine is presented. Analysis showed correlation between parent acid, but no with acid. Identification associations was aided by examining chemically sensible subgroups set, this approach highlighted significantly different relationships these subgroups. Thus, example, expected negative found 24 anhydrous benzoate salts, a positive observed eight halide salts....
This paper describes the application of a novel antisolvent crystallization approach to rapid production tunable solid solutions hydrophobic amino acids, comprising l-leucine, l-isoleucine, and l-valine. The provides an alternative other routes, e.g., ball-milling, liquid-assisted grinding, slurry methods, achieve required multicomponent phases. We report new crystal structures l-leucine/l-isoleucine l-leucine/l-valine, confirm recent on form l-isoleucine/l-valine. used these complexes as...
Methionyl-tRNA synthetase (MetRS) is a chemically validated drug target in kinetoplastid parasites Trypanosoma brucei and Leishmania donovani. To date, all MetRS inhibitors described bind similar way to an expanded methionine pocket adjacent, auxiliary pocket. In the current study, we have identified structurally novel class of containing 4,6-diamino-substituted pyrazolopyrimidine core (the MetRS02 series). Crystallographic studies revealed that compounds allosteric L. major not previously...
ABSTRACT After the Scottish Prison Service (SPS) introduced mail photocopying procedures in December 2021, a shift smuggling methods was observed for synthetic cannabinoid receptor agonists (SCRAs) and other new psychoactive substances (NPS) from drug‐infused papers back to traditional sample matrices (e.g., tablets powders), although also emerged. This study reports on waxy‐ or putty‐like materials as novel drug preparation SCRAs drugs seized UK prisons. In 2023, 22 of these preparations...