Synthesis of 8-geranyloxypsoralen analogues and their evaluation as inhibitors of CYP3A4.
- E. Row, S. A. Brown, A. Stachulski, M. Lennard
- Chemistry, BiologyBioorganic & Medicinal Chemistry
- 1 June 2006
Design, synthesis and evaluation of furanocoumarin monomers as inhibitors of CYP3A4.
- E. Row, S. A. Brown, A. Stachulski, M. Lennard
- Chemistry, BiologyOrganic and biomolecular chemistry
- 7 April 2006
A range of analogues based on bergamottin are designed and synthesised to investigate the relationship between chemical structure and inhibition of CYP3A4 activity and it is suggested that this functional group is key to the interaction between these compounds and CYP 3A4.
DEVELOPMENT OF NOVEL FURANOCOUMARIN DIMERS AS POTENT AND SELECTIVE INHIBITORS OF CYP3A4
- E. Row, S. A. Brown, A. Stachulski, M. Lennard
- Biology, ChemistryDrug Metabolism And Disposition
- 1 February 2006
All the dimers tested were extremely potent inhibitors of CYP3A4 activity, and in particular, dimer 55EE was highly selective toward the enzyme, suggesting that this compound is a suitable probe for determining the contribution of CYp3A 4 to drug metabolism.
Thiazolides as novel antiviral agents. 1. Inhibition of hepatitis B virus replication.
- A. Stachulski, C. Pidathala, J. Rossignol
- Chemistry, BiologyJournal of Medicinal Chemistry
- 23 June 2011
The syntheses and activities of a wide range of thiazolides against hepatitis B virus replication are reported, with QSAR analysis of results showing a good correlation of observed EC(90) for intracellular virions withThiazolide structural parameters.
Identification of isoflavone derivatives as effective anticryptosporidial agents in vitro and in vivo.
- A. Stachulski, N. Berry, J. Rossignol
- BiologyJournal of Medicinal Chemistry
- 25 January 2006
We report the preparation and antiparasitic activity in vitro and in vivo of a series of isoflavone derivatives related to genistein. These analogues retain the 5,7-dihydroxyisoflavone core of…
Thiazolides as novel antiviral agents. 2. Inhibition of hepatitis C virus replication.
- A. Stachulski, C. Pidathala, J. Rossignol
- Biology, ChemistryJournal of Medicinal Chemistry
- 2011
It is shown here that the 5'-Cl analogue 4 has closely comparable in vitro activity and a good cell safety index, and updated the mode of action of the thiazolides and explain the candidate selection that has led to compound 4 entering preclinical development.
An alkynylboronate cycloaddition strategy to functionalised benzyne derivatives.
- J. Kirkham, Patrick M. Delaney, G. Ellames, E. Row, J. Harrity
- Chemistry, BiologyChemical Communications
- 28 July 2010
A new approach to benzyne precursors has been developed that involves the [4+2] cycloaddition of trimethylsilyl alkynylboronates with 2-pyrones, followed by oxidation and trifluoromethylsulfonylation…
Second-generation nitazoxanide derivatives: thiazolides are effective inhibitors of the influenza A virus.
- A. Stachulski, M. Santoro, J. Rossignol
- Chemistry, BiologyFuture Medicinal Chemistry
- 9 April 2018
A range of thiazolides show useful activity against an H1N1 strain of IAV, and further evaluation of these molecules as potential new small molecule therapies is justified.
Investigation of the Origins of Regiochemical Control in [4+2] Cycloadditions of 2-Pyrones and Alkynylboronates
- J. Kirkham, A. Leach, E. Row, J. Harrity
- Chemistry, Biology
- 1 July 2012
The [4+2] cycloaddition of 2-pyrones with substituted alkynylboronates has been studied and mechanisms suggest that the high regioselectivity observed is due to stabilization of a zwitterionic transition state.
Synthetic approaches to regiospecifically mono‐ and dilabelled arenes
- Thomas J. Gregson, J. Herbert, E. Row
- Chemistry, Environmental Science
- 26 July 2011
A variety of methods for the preparation of selectively mono-, di- or tri-labelled arenes are reviewed. The review concentrates on those for which the application to labelled synthesis has been…
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