Here we report the discovery, by high-throughput screening, of three novel (2-amino-5-keto)thiazole
compounds that act as selective potentiators of nicotinic acetylcholine receptors. …

The analogues 2, 3, 8a-c, 9, 13, and 14 of the d-carboline 6-(benzyloxy)-4-(methoxymethyl)-|
8-carboline-3-carboxylic acid ethyl ester (ZK-93423, 1) were synthesized in order to …

Transmembrane AMPA receptor regulatory proteins (TARPs) are a family of scaffolding
proteins that regulate AMPA receptor trafficking and function. TARP γ-8 is one member of this …

The factors that control the relative and absolute stereochemistry of 1,3-disubstituted and 1,2,3-trisubstituted
tetrahydro-β-carbolines formed via the Pictet–Spengler reaction are …

A focused screening strategy identified thienopyrimidine 12 as a cannabinoid receptor type
2 agonist (hCB2) with moderate selectivity over the hCB1 receptor. This initial hit suffered …

Tricyclic isoxazoles were identified from a screen as a novel class of selective multidrug
resistance protein (MRP1) inhibitors. From a screen lead, SAR efforts resulted in the preparation …

A series of analogues of the protein kinase C (PKC) inhibitory natural product balanol which
bear modified benzophenone subunits are described. The analogues were designed with …

A series of balanol analogs in which the perhydroazepine ring and the p-hydroxybenzamide
moiety were combined into an acyclic linked unit have been prepared and evaluated for …

… Patrick D Bailey,* Sean P Hollinshead and Neil R McLay … This reaction in refluxing
benzene (Dean-Stark water extraction) was catalysed by p-TsOH; … Campos, P. Mokry, JM …

Regio- and stereoisomeric indane analogs (4–6) of balanol (−)-1, a potent protein kinase C (PKC)
inhibitor, were synthesized in which the perhydroazepine of balanol was replaced by …