Graeme Irvine Stevenson

2-Aryl tryptamines: selective high-affinity antagonists for the h5-HT2A receptor

A series of 2-aryl tryptamines have been identified as high-affinity h5-HT2A antagonists. Structure-activity relationship studies have shown that h5-HT2A affinity can be attained via modifications to the tryptamine side chain and that selectivity over h5-HT2C and hD2 receptors can be controlled by suitable C-2 aryl groups.

Traceless solid phase synthesis of 2,3-disubstituted indoles

Abstract An efficient method for the traceless solid phase synthesis of 2,3-disubstituted indoles using a THP linker and a Pd(0)-mediated annulation of 2-iodoaniline and acetylenes is reported.

Solid-phase synthesis of 2,3-disubstituted indoles: discovery of a novel, high-affinity, selective h5-HT2A antagonist.

The application of a novel solid-phase synthesis of 2,3-disubstituted indoles utilizing a carbamate indole linker is described resulting in the identification of the novel, high-affinity, selective h5-HT2A antagonist 19.

Amino acid bioisosteres: design of 2-quinolone derivatives as glycine-site N-methyl-D-aspartate receptor antagonists

Abstract 3-Substituted-2-quinoloners ( 6–8 ) have been identified as glycine-site N-methyl-D-aspartate receptor antagonists. It is proposed that the α-phenyl lactam unit in the potent 4-hydroxy-3-phenyl derivatives ( 7d and 8b , L-701,315) may act as a glycine bioisostere in receptor recognition.

Serine derived NK1 antagonists 2: a pharmacophore model for arylsulfonamide binding

Modifications to the spirocyclic aryl sulfonamide portion of serine derived NK1 antagonists allow a partial pharmacophore model to be developed.

Serine derived NK1 antagonists. 1: The effect of modifications to the serine substituents.

A series of novel serine derived NK1 antagonists is described. The effect of variations in the N-benzyl, O-benzyl and serine groups are used to define the elements which are necessary for binding.

Synthesis of cis and trans 4-amido 2-carboxytetrahydroquinolines, high affinity ligands at the glycine site of the NMDA receptor

N-Arylimino esters (3) react with enamides (4) under Lewis acid catalysis to afford cis 4-amido-2-carboxytetrahydroquinolines (5). The products of this reaction are easily converted to the biologically active trans conformers. Introduction of substituents at C-3 has no effect on affinity at the Glycine site of the NMDA receptor.