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Inhibition of neuronal GABA uptake and glial beta-alanine uptake by synthetic GABA analogues.
TLDR
The results confirm that both uptake processes favour a substantially folded conformation in GABA and β-alanine, and analogues with long alkyl side chain substituents were significantly inhibited. Expand
GABA analogues: conformational analysis of effects on [3H]GABA binding to postsynaptic receptors in human cerebellum
TLDR
Early structure-activity relationship studies of post-synaptic GABA rcceptors in mammalian CNS and in invertebrates showed that a positively charged and a negatively charged or polarised group about 6 A apart on a molecule that possesses some conformational flexibility are requirements for GABA binding. Expand
Marine steroids. Part III. On the structure of marthasterone glucoside, from the starfish Marthasterais glacialis.
A 1H n.m.r. method based on the chemical shift of the 10-methyl protons is used to locate the position of the glucose residue in marthasterone 6α-glucoside, which is characterised as itsExpand
Inhibition of [3H]GABA Binding to Postsynaptic Receptors in Human Cerebellar Synaptic Membranes by Carboxyl and Amino Derivatives of GABA
TLDR
It was concluded that a pyramidal nitrogen atom is favoured for binding of GABA analogues to human cerebellar membranes because it can interact with the postsynaptic membrane. Expand
Specific inhibitors in vitamin biosynthesis. Part 7. Syntheses of blocked 7,8-dihydropteridines viaα-amino ketones
The synthesis of 15 blocked 7,8-dihydropteridines is described in which the pyrazine ring is built from a derivative of an α-amino ketone. Three routes to the amino ketones based upon amino acids,Expand
Specific inhibitors in vitamin biosynthesis. Part 8. Syntheses of some functionalised 7,7-dialkyl-7,8-dihydropterins
The synthesis of a variety of functionalised blocked 7,8-dihydropteridines is described. The functional groups were chosen to provide compounds with potential for investigating the protein chemistryExpand
Specific inhibitors in vitamin biosynthesis. Part 9. Reactions of 7,7-dialkyl-7,8-dihydropteridines of use in the synthesis of potential inhibitors of tetrahydrofolate biosynthesis
Reactions of 7,7-dialkyl-7,8-dihydropteridines which are of potential use in modifying substituents on the pyrazine ring to yield compounds with inhibitory activity againstExpand
Steroid conjugates. Part V. Glucuronosides of 19-oxygenated 3β-hydroxyandrost-5-en-17-ones
The monoglucuronosides of 19-hydroxy- and 19-oxo-3β-hydroxyandrost-5-en-17-one have been prepared by the Koenigs–Knorr procedure. Steiic effects in these reactions are compared with those encounteredExpand
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