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Andrew Stachulski

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Andrew V Stachulski; Xiaoli Meng
Glucuronides from metabolites to medicines: a survey of the in vivo generation, chemical synthesis and properties of glucuronides.
Emma-Claire Elliott; James L Maggs; B Kevin Park; Laura J Parry; Sophie L Regan; Elizabeth R Bowkett; Dominic P Williams; Andrew V Stachulski
Haloarene derivatives of carbamazepine with reduced bioactivation liabilities: 2-monohalo and 2,8-dihalo derivatives.
Emma-Claire Elliott; James L Maggs; Paul M O'Neill; B Kevin Park; Sophie L Regan; John Bacsa; Elizabeth R Bowkett; Andrew V Stachulski
Convenient syntheses of benzo-fluorinated dibenz[b,f]azepines: rearrangements of isatins, acridines, and indoles.

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All Publications

2013: Andrew V Stachulski; Xiaoli Meng
Glucuronides from metabolites to medicines: a survey of the in vivo generation, chemical synthesis and properties of glucuronides.
Natural product reports 2013;30(6):806-48.
2012: Emma-Claire Elliott; James L Maggs; B Kevin Park; Laura J Parry; Sophie L Regan; Elizabeth R Bowkett; Dominic P Williams; Andrew V Stachulski
Haloarene derivatives of carbamazepine with reduced bioactivation liabilities: 2-monohalo and 2,8-dihalo derivatives.
Journal of medicinal chemistry 2012;55(22):9773-84.
2011: Emma-Claire Elliott; James L Maggs; Paul M O'Neill; B Kevin Park; Sophie L Regan; John Bacsa; Elizabeth R Bowkett; Andrew V Stachulski
Convenient syntheses of benzo-fluorinated dibenz[b,f]azepines: rearrangements of isatins, acridines, and indoles.
Organic letters 2011;13(20):5592-5.
2011: Xiaoli Meng; Dean J Naisbitt; Munir Pirmohamed; Andrew V Stachulski; Neil G Berry; John Farrell; Neil S French; Rosalind E Jenkins; Catherine S Lane; James L Maggs; B Kevin Park
Direct evidence for the formation of diastereoisomeric benzylpenicilloyl haptens from benzylpenicillin and benzylpenicillenic acid in patients.
The Journal of pharmacology and experimental therapeutics 2011;338(3):841-9.
2011: Andrew V Stachulski; Eleanor Row; J Edward Semple; Raman Sharma; Sarah A Allman; Joanne Bentley; Neil G Berry; Geoffrey Edwards; Jennifer Hellier; Alison Helm; Mazhar Iqbal; Brent E Korba; Chandrakala Pidathala; Jean-François Rossignol
Thiazolides as novel antiviral agents. 1. Inhibition of hepatitis B virus replication.
Journal of medicinal chemistry 2011;54(12):4119-32.
2011: Andrew V Stachulski
Chemistry and reactivity of acyl glucuronides.
Current drug metabolism 2011;12(3):215-21.
2011: Lisa Iddon; Selena E Richards; Caroline Johnson; John R Harding; Ian D Wilson; Jeremy K Nicholson; John C Lindon; Andrew V Stachulski
Synthesis of a series of phenylacetic acid 1-β-O-acyl glucosides and comparison of their acyl migration and hydrolysis kinetics with the corresponding acyl glucuronides.
Organic & biomolecular chemistry 2011;9(3):926-34.
2010: Elin S Karlsson; Caroline Johnson; Sunil Sarda; Lisa Iddon; Mazhar Iqbal; Xiaoli Meng; John R Harding; Andrew V Stachulski; Jeremy K Nicholson; Ian D Wilson; John C Lindon
High-performance liquid chromatography/mass spectrometric and proton nuclear magnetic resonance spectroscopic studies of the transacylation and hydrolysis of the acyl glucuronides of a series of phenylacetic acids in buffer and human plasma.
Rapid communications in mass spectrometry : RCM 2010;24(20):3043-51.
2010: Richard Amewu; Peter Gibbons; Amira Mukhtar; Andrew V Stachulski; Stephen A Ward; Charlotte Hall; Karen Rimmer; Jill Davies; Livia Vivas; John Bacsa; Amy Mercer; Gemma Nixon; Paul A Stocks; Paul M O'Neill
Synthesis, in vitro and in vivo antimalarial assessment of sulfide, sulfone and vinyl amide-substituted 1,2,4-trioxanes prepared via thiol-olefin co-oxygenation (TOCO) of allylic alcohols.
Organic & biomolecular chemistry 2010;8(9):2068-77.
2010: Gilles Gargala; Laetitia Le Goff; Jean Jacques Ballet; Loïc Favennec; Andrew V Stachulski; Jean-François Rossignol
Evaluation of new thiazolide/thiadiazolide derivatives reveals nitro group-independent efficacy against in vitro development of Cryptosporidium parvum.
Antimicrobial agents and chemotherapy 2010;54(3):1315-8.
2010: Bénédicte Pacorel; Suet C Leung; Andrew V Stachulski; Jill Davies; Livia Vivas; Hollie Lander; Stephen A Ward; Marcel Kaiser; Reto Brun; Paul M O'Neill
Modular synthesis and in vitro and in vivo antimalarial assessment of C-10 pyrrole mannich base derivatives of artemisinin.
Journal of medicinal chemistry 2010;53(2):633-40.
2010: Caroline Johnson; E Karlsson; S Sarda; L Iddon; Mazhar Iqbal; X Meng; John R Harding; Andrew V Stachulski; Jeremy K Nicholson; Ian D Wilson; John C Lindon
Integrated HPLC-MS and (1)H-NMR spectroscopic studies on acyl migration reaction kinetics of model drug ester glucuronides.
Xenobiotica; the fate of foreign compounds in biological systems 2010;40(1):9-23.
2009: Derren J Heyes; Colin Levy; Pierre Lafite; Ian S Roberts; Marie Goldrick; Andrew V Stachulski; Steven B Rossington; Deborah Stanford; Stephen E J Rigby; Nigel S Scrutton; David Leys
Structure-based mechanism of CMP-2-keto-3-deoxymanno-octulonic acid synthetase: convergent evolution of a sugar-activating enzyme with DNA/RNA polymerases.
The Journal of biological chemistry 2009;284(51):35514-23.
2009: Lee Bollans; John Bacsa; Jonathan A Iggo; Gareth A Morris; Andrew V Stachulski
The acyl nitroso Diels-Alder (ANDA) reaction of sorbate derivatives: an X-ray and 15N NMR study with an application to amino-acid synthesis.
Organic & biomolecular chemistry 2009;7(21):4531-8.
2009: Neil G Berry; Lisa Iddon; Mazhar Iqbal; Xiaoli Meng; Prabha Jayapal; Caroline Johnson; Jeremy K Nicholson; John C Lindon; John R Harding; Ian D Wilson; Andrew V Stachulski
Synthesis, transacylation kinetics and computational chemistry of a set of arylacetic acid 1beta-O-acyl glucuronides.
Organic & biomolecular chemistry 2009;7(12):2525-33.
2008: Caroline Johnson; Toby J Athersuch; Ian D Wilson; Lisa Iddon; Xiaoli Meng; Andrew V Stachulski; John C Lindon; Jeremy K Nicholson
Kinetic and J-resolved statistical total correlation NMR spectroscopy approaches to structural information recovery in complex reacting mixtures: application to acyl glucuronide intramolecular transacylation reactions.
Analytical chemistry 2008;80(13):4886-95.
2007: Xiaoli Meng; James L Maggs; David C Pryde; Simon Planken; Rosalind E Jenkins; Torren M Peakman; Kevin Beaumont; Christopher Kohl; B Kevin Park; Andrew V Stachulski
Cyclization of the acyl glucuronide metabolite of a neutral endopeptidase inhibitor to an electrophilic glutarimide: synthesis, reactivity, and mechanistic analysis.
Journal of medicinal chemistry 2007;50(24):6165-76.
2007: Caroline Johnson; Ian D Wilson; John R Harding; Andrew V Stachulski; Lisa Iddon; Jeremy K Nicholson; John C Lindon
NMR spectroscopic studies on the in vitro acyl glucuronide migration kinetics of Ibuprofen ((+/-)-(R,S)-2-(4-isobutylphenyl) propanoic acid), its metabolites, and analogues.
Analytical chemistry 2007;79(22):8720-7.
2007: Dean J Naisbitt; Louise S Sanderson; Xiaoli Meng; Andrew V Stachulski; Stephen E Clarke; B Kevin Park
Investigation of the immunogenicity of diclofenac and diclofenac metabolites.
Toxicology letters 2007;168(1):45-50.
2007: Andrew V Stachulski
The chemistry and biological activity of acyl glucuronides.
Current opinion in drug discovery & development 2007;10(1):58-66.
2006: Richard Amewu; Andrew V Stachulski; Stephen A Ward; Neil G Berry; Patrick G Bray; Jill Davies; Gael Labat; Livia Vivas; Paul M O'Neill
Design and synthesis of orally active dispiro 1,2,4,5-tetraoxanes; synthetic antimalarials with superior activity to artemisinin.
Organic & biomolecular chemistry 2006;4(24):4431-6.
2006: Richard Amewu; Andrew V Stachulski; Neil G Berry; Stephen A Ward; Jill Davies; Gael Labat; Jean-François Rossignol; Paul M O'Neill
Synthesis of 1,2,4-trioxepanes via application of thiol-olefin co-oxygenation methodology.
Bioorganic & medicinal chemistry letters 2006;16(23):6124-30.
2006: Andrew V Stachulski; John R Harding; John C Lindon; James L Maggs; B Kevin Park; Ian D Wilson
Acyl glucuronides: biological activity, chemical reactivity, and chemical synthesis.
Journal of medicinal chemistry 2006;49(24):6931-45.
2006: Ying Wu; Joseph Sanderson; John Farrell; Nicola S Drummond; Anita Hanson; Elizabeth Bowkett; Neil Berry; Andrew V Stachulski; Stephen E Clarke; Werner J Pichler; Munir Pirmohamed; B Kevin Park; Dean J Naisbitt
Activation of T cells by carbamazepine and carbamazepine metabolites.
The Journal of allergy and clinical immunology 2006;118(1):233-41.
2006: Eleanor Row; SA Brown; Andrew V Stachulski; Martin S Lennard
Synthesis of 8-geranyloxypsoralen analogues and their evaluation as inhibitors of CYP3A4.
Bioorganic & medicinal chemistry 2006;14(11):3865-71.
2006: Eleanor Row; SA Brown; Andrew V Stachulski; Martin S Lennard
Design, synthesis and evaluation of furanocoumarin monomers as inhibitors of CYP3A4.
Organic & biomolecular chemistry 2006;4(8):1604-10.
2006: Andrew V Stachulski; Neil G Berry; A C Lilian Low; Shelley L Moores; Eleanor Row; david charles warhurst; Ipemida S Adagu; Jean-François Rossignol
Identification of isoflavone derivatives as effective anticryptosporidial agents in vitro and in vivo.
Journal of medicinal chemistry 2006;49(4):1450-4.
2006: Eleanor Row; SA Brown; Andrew V Stachulski; Martin S Lennard
Development of novel furanocoumarin dimers as potent and selective inhibitors of CYP3A4.
Drug metabolism and disposition: the biological fate of chemicals 2006;34(2):324-30.
2005: Jennifer A Perrie; John R Harding; David W Holt; Atholl Johnston; Paul Meath; Andrew V Stachulski
Effective synthesis of 1beta-acyl glucuronides by selective acylation.
Organic letters 2005;7(13):2591-4.
2005: John R Harding; Clare D King; Jennifer A Perrie; Deborah Sinnott; Andrew V Stachulski
Glucuronidation of steroidal alcohols using iodosugar and imidate donors.
Organic & biomolecular chemistry 2005;3(8):1501-7.
2004: Jane R Kenny; James L Maggs; Xiaoli Meng; Deborah Sinnott; Stephen E Clarke; B Kevin Park; Andrew V Stachulski
Syntheses and characterization of the acyl glucuronide and hydroxy metabolites of diclofenac.
Journal of medicinal chemistry 2004;47(11):2816-25.
2004: Ying-Kit Chung; Timothy D W Claridge; George W J Fleet; Stephen W Johnson; John H Jones; Keith W Lumbard; Andrew V Stachulski
An unsaturated peptidomimetic assembly derived from a carbohydrate.
Journal of peptide science : an official publication of the European Peptide Society 2004;10(1):1-7.
2003: Jennifer A Perrie; John R Harding; Clare King; Deborah Sinnott; Andrew V Stachulski
Glycosidation with a disarmed glycosyl iodide: promotion and scope.
Organic letters 2003;5(24):4545-8.
2003: Jamie Bickley; Jennifer A Cottrell; John R Ferguson; Robert A Field; John R Harding; David L Hughes; K P Ravindranathan Kartha; Jayne L Law; Feodor Scheinmann; Andrew V Stachulski
Preparation, X-ray structure and reactivity of a stable glycosyl iodide.
Chemical communications (Cambridge, England) 2003;(11):1266-7.
2003: Andrew V Stachulski; Feodor Scheinmann; John R Ferguson; Jayne L Law; Keith W Lumbard; Peter Hopkins; Naina Patel; Simon Clarke; Anna Gloyne; Simon P Joel
Structure-activity relationships of some opiate glycosides.
Bioorganic & medicinal chemistry letters 2003;13(6):1207-14.
2001: Paul M O'Neill; Feodor Scheinmann; Andrew V Stachulski; James L Maggs; B Kevin Park
Efficient preparations of the beta-glucuronides of dihydroartemisinin and structural confirmation of the human glucuronide metabolite.
Journal of medicinal chemistry 2001;44(9):1467-70.
2001: Paul M O'Neill; A Miller; Laurence P D Bishop; Stephen Hindley; James L Maggs; Stephen A Ward; S M Roberts; Feodor Scheinmann; Andrew V Stachulski; G H Posner; B Kevin Park
Synthesis, antimalarial activity, biomimetic iron(II) chemistry, and in vivo metabolism of novel, potent C-10-phenoxy derivatives of dihydroartemisinin.
Journal of medicinal chemistry 2001;44(1):58-68.