A5089300509- Chemical Synthesis and Analysis
- S100 Proteins and Annexins
- Synthesis and Biological Evaluation
- Nitric Oxide and Endothelin Effects
- Eicosanoids and Hypertension Pharmacology
- Synthesis and Reactions of Organic Compounds
- Synthesis and Catalytic Reactions
- Asymmetric Synthesis and Catalysis
- Chemical Synthesis and Reactions
- ATP Synthase and ATPases Research
- Bioactive Compounds and Antitumor Agents
- Advanced Glycation End Products research
- Click Chemistry and Applications
- Inflammation biomarkers and pathways
- Antimicrobial agents and applications
- Antimicrobial Peptides and Activities
- Hormonal Regulation and Hypertension
- Carbon dioxide utilization in catalysis
- Chemical Reaction Mechanisms
- Hormonal and reproductive studies
- Synthesis of β-Lactam Compounds
- Computational Drug Discovery Methods
- Polyamine Metabolism and Applications
- Genomics, phytochemicals, and oxidative stress
- Cancer Research and Treatments
University of Hertfordshire
2008-2021
University College London
2004-2007
King's College London
2003-2005
University of Exeter
2005
Wolfson Foundation
2004-2005
The Royal Free Hospital
2004
Middlesex Hospital
2004
Mount Vernon Hospital
2002-2003
Western General Hospital
1992-1995
University of Edinburgh
1995
The enzyme DDAH metabolizes methylarginines that are inhibitors of nitric oxide synthase (NOS). Substrate-based mammalian have been synthesized, with optimization to give selective inhibition no significant direct effect on NOSs. These the first examples reversible activity and selectivity. In vivo administration increases plasma ADMA levels, giving proof concept these can be used probe physiological effects inhibition, potential for pharmaceutical use in diseases where excess NO production...
S100P, a calcium-binding protein, is known to advance tumor progression and metastasis in pancreatic several other cancers. Herein described the silico identification of putative binding pocket S100P identify, synthesize evaluate novel small molecules with potential selectively bind inhibit its activation cell survival metastatic pathways. The virtual screening drug-like database against model led over 100 clusters diverse scaffolds. A representative test set identified number structurally...
Evidence that nitric oxide (NO) is involved in cytokine-mediated islet β-cell dysfunction and destruction vitro has led to the hypothesis increased production of NO may contribute pathogenesis insulin-dependent diabetes mellitus (IDDM). This study demonstrates oral administration Nω-nitro-L-arginine methyl ester (an inhibitor synthase) from 30 150 days age significantly reduced (P < 0.05) incidence IDDM diabetes-prone BB/E rats. supports idea plays a significant role this animal model.
The synthesis of the quinoline alkaloid atanine 6, by selective demethylation 2,4-dimethoxyquinoline 11 is presented. An alternative utilising a thiolate anion leads to regioisomeric 4-hydroxyquinoline 13.
A range of pentafluorophenyl (PFP) sulfonate esters derived from the reaction PFP vinyl and various nitrones are shown to have significant inhibitory activity against bacterial enzymes DDAH ADI.
A N-derivatized 3-dimethylaminopropyloxypyrazole library was prepared using solution-phase parallel synthesis. The designed physicochemical constraints to remove non-membrane-permeable molecules. Cupric acetate-mediated N-arylation with aryl boronic acids proceeded regioselectively form the N-2-substituted derivatives. presence of 3-dimethylaminopropyloxy group found completely control regioselectivity arylation. Presence a dimethylaminoethyloxy or dimethylaminobutyloxy gave lesser degree...
Cationic peptides with antimicrobial properties are ubiquitous in nature and have been studied for many years an attempt to design novel antibiotics. However, very few molecules used the clinic so far, sometimes due their complexity but, mostly, as a consequence of unfavorable pharmacokinetic profile associated peptides. The aim this work is investigate cationic order identify common structural features which could be useful small or peptido-mimetics improved drug-like activity against Gram...
Cationic antimicrobial peptides have attracted interest, both as agents and for their ability to increase cell permeability potentiate other antibiotics. However, toxicity mammalian cells complexity hindered development clinical use. We present the design synthesis of very short cationic (3–9 residues) with potential dual bacterial membrane permeation efflux pump inhibition functionality. Peptides were designed based upon in silico similarity known active inhibitors. A number these activity...
Oxidation of indole-3-acetic acid and its derivatives by peroxidases such as that from horseradish produces many products, including 3-methylene-2-oxindoles. These have long been associated with biological activity, but their reactivity has not characterized. We previously demonstrated the potential value substituted indole acetic acids peroxidase basis for targeted cancer therapy, since compounds are low cytotoxicity until oxidized, when high is observed; combination prodrug enzyme depletes...
ABSTRACT Serotoninergic control of aldosterone secretion in vivo was investigated conscious rats with indwelling arterial cannulae. Serial blood samples were taken from the animals before and after i.p. administration 1 ml (4 g/l) 5-hydroxytryptophan (5-HTP), precursor serotonin, or saline they analysed for 5-HTP, 5-hydroxyindoleacetic acid, plasma renin activity (PRA), corticosterone, aldosterone, sodium potassium concentrations. The role renin-angiotensin system pretreated week...
Oxidative stress plays an important role in the pathogenesis of chronic obstructive pulmonary disease (COPD). COPD is one leading causes mortality UK. Current treatment options for are limited and do not prevent progression. Hence, there urgent requirement alternative novel therapeutic approaches. Stilbenoid natural products, including trans-resveratrol synthetic analogues have demonstrated a variety biological properties, particular anti-oxidant anti-inflammatory properties. Cell health...
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