Activation of T cells by carbamazepine and carbamazepine metabolites.
Direct Evidence for the Formation of Diastereoisomeric Benzylpenicilloyl Haptens from Benzylpenicillin and Benzylpenicillenic Acid in Patients
- X. Meng, R. Jenkins, B. K. Park
- Biology, ChemistryJournal of Pharmacology and Experimental…
- 1 September 2011
PA was found to be more potent than BP with respect to stimulation of T cells from patients with penicillin hypersensitivity, illustrating the functional relevance of diastereoisomeric hapten formation.
Acyl glucuronides: biological activity, chemical reactivity, and chemical synthesis.
Syntheses and characterization of the acyl glucuronide and hydroxy metabolites of diclofenac.
In humans, metabolism of the commonly used nonsteroidal antiinflammatory drug diclofenac 1 yields principally the 4'-hydroxy 2, 5-hydroxy 3, and acyl glucuronide 4 metabolites. All three metabolites…
The Generation, Detection, and Effects of Reactive Drug Metabolites
- A. Stachulski, T. Baillie, M. Lennard
- Biology, ChemistryMedicinal research reviews (Print)
- 1 September 2013
A critique of protein‐reactive metabolites, not linked conclusively to a toxic event, is presented and the impact of such data on the drug discovery process is discussed, both through early detection of reactive metabolites and informed synthetic design, which eliminates unfavorable functionality from drug candidates.
NMR spectroscopic studies on the in vitro acyl glucuronide migration kinetics of Ibuprofen ((+/-)-(R,S)-2-(4-isobutylphenyl) propanoic acid), its metabolites, and analogues.
It is shown that the (R)- and (S)-ibuprofen AGs have different transacylation properties, and the implications of these findings are discussed in terms of structure-activity relationships.
The use of the N(π)-phenacyl group for the protection of the histidine side chain in peptide synthesis
The practicability of the N(π)-phenacyl protective group has been demonstrated in a synthesis of thyroliberin and under carboxy-activating conditions which cause gross racemisation of (5) yields optically pure peptide.
Synthesis of 8-geranyloxypsoralen analogues and their evaluation as inhibitors of CYP3A4.
Rational Design, Synthesis, and Biological Evaluation of Heterocyclic Quinolones Targeting the Respiratory Chain of Mycobacterium tuberculosis.
A high-throughput screen (HTS) was undertaken against the respiratory chain dehydrogenase component, NADH:menaquinone oxidoreductase (Ndh) of Mycobacterium tuberculosis (Mtb). The 11000 compounds…
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.