Stachulski, Andrew - University of Liverpool

个人简介

I have been nominated for an Industrial Carbohydrate Chemistry award by my AstraZeneca colleagues. (RSC. Outcome expected June 2007. 2007)

研究领域

The Romark Centre for Drug Discovery was established in this Department in 2004. Funded by Romark LC of Tampa, USA, we are engaged in the design and synthesis of new antiinfective agents, with the main current emphasis on antivirals. Natural Product Chemistry: Carbohydrate chemistry is a major interest of the group. In particular new methods of glycosidation using glycosyl iodides have been developed and selective acylation has been exploited in an efficient new synthesis of acyl glucuronides. Other carbohydrate interests are the synthesis of novel carbohydrate-based antibacterials and pyranose-based carbopeptoids. Metabolism: We collaborate with Kevin Park’s group in Pharmacology and with major pharmaceutical companies in the application of chemical synthesis to issues of drug metabolism and potential toxicity. Here again the synthesis of glucuronides, especially acyl glucuronides, is an important feature.

近期论文

查看导师新发文章（温馨提示：请注意重名现象，建议点开原文通过作者单位确认）

Synthesis and pre-clinical studies of new amino-acid ester thiazolide prodrugs Dissecting the reaction of Phase II metabolites of ibuprofen and other NSAIDS with human plasma protein Mass Spectrometric Characterization of Circulating Covalent Protein Adducts Derived from a Drug Acyl Glucuronide Metabolite: Multiple Albumin Adductions in Diclofenac Patients Direct Evidence for the Formation of Diastereoisomeric Benzylpenicilloyl Haptens from Benzylpenicillin and Benzylpenicillenic Acid in Patients Thiazolides as Novel Antiviral Agents. 1. Inhibition of Hepatitis B Virus Replication 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 The acyl nitroso Diels–Alder (ANDA) reaction of sorbate derivatives: an X-ray and 15N NMR study with an application to amino-acid synthesis Convenient syntheses of deoxypyranose sugars from glucuronolactone Cyclization of the Acyl Glucuronide Metabolite of a Neutral Endopeptidase Inhibitor to an Electrophilic Glutarimide: Synthesis, Reactivity, and Mechanistic Analysis Efficient synthesis of 1β-O-acyl glucuronides via selective acylation of allyl or benzyl d-glucuronate Investigation of the immunogenicity of diclofenac and diclofenac metabolites NMR Spectroscopic Studies on the in Vitro Acyl Glucuronide Migration Kinetics of Ibuprofen ((±)-( R , S )-2-(4-Isobutylphenyl) Propanoic Acid), Its Metabolites, and Analogues The chemistry and biological activity of acyl glucuronides Acyl Glucuronides: Biological Activity, Chemical Reactivity, and Chemical Synthesis DEVELOPMENT OF NOVEL FURANOCOUMARIN DIMERS AS POTENT AND SELECTIVE INHIBITORS OF CYP3A4 Design and synthesis of orally active dispiro 1,2,4,5-tetraoxanes; synthetic antimalarials with superior activity to artemisinin Design, synthesis and evaluation of furanocoumarin monomers as inhibitors of CYP3A4 Identification of Isoflavone Derivatives as Effective Anticryptosporidial Agents in Vitro and in Vivo Synthesis of 1,2,4-trioxepanes via application of thiol-olefin Co-oxygenation methodology Synthesis of 8-geranyloxypsoralen analogues and their evaluation as inhibitors of CYP3A4 Effective Synthesis of 1β-Acyl Glucuronides by Selective Acylation Glucuronidation of steroidal alcohols using iodosugar and imidate donors In Vitro Efficacies of Nitazoxanide and Other Thiazolides against Neospora caninum Tachyzoites Reveal Antiparasitic Activity Independent of the Nitro Group New stable anomeric hydroperoxides derived from 2-deoxysugars; enantioselective epoxidation of 2-methyl-1,4-naphthoquinone The design and synthesis of novel anomeric hydroperoxides: influence of the carbohydrate residue in the enantioselective epoxidation of quinones