Chandra R. Shah

TL;DR: High throughput screening, using the recombinant human H(3) receptor, was used to identify novel histamine H( 3) receptor antagonists that afforded potent, selective, orally bioavailable compounds with favorable blood-brain barrier penetration.

TL;DR: In this paper, the authors describe macroheterocyclic compounds useful as kinase or dual-kinase inhibitors, methods for producing such compounds, and methods for treating or ameliorating a kinase/dualkinase mediated disorder.

TL;DR: A series of small molecules consisting of a heterocyclic core flanked by two basic functionalities were synthesized and screened for in vitro affinity at the human histamine H(3) receptor and one member was found to be a high affinity, selective antagonist that crosses the blood-brain barrier and occupies H( 3) receptors after oral administration in the rat.

TL;DR: Optimization of the physical properties of these histamine H3 antagonists led to the discovery of several promising lead compounds, and extensive preclinical profiling aided in the identification of compounds with optimal duration of action for wake promoting activity.