41 research outputs found
Enantioselective Synthesis of the Bottom Half of Chlorotricholide. 3. Studies of the Steric Directing Group Strategy for Stereocontrol in Intramolecular Diels-Alder Reactions
No full textCharacterization of the Antiviral Activity of Highly Substituted Pyrroles: A Novel Class of Non-Nucleoside HIV-1 Reverse Transcriptase Inhibitor
No full text
A diol-functionalized ionic liquid: an efficient, simple, and recoverable “capture and release” reagent for aldehydes
No full textAmino-Functionalized Ionic Liquid as A Nucleophilic Scavenger in Solution Phase Combinatorial Synthesis
No full text
The discovery and optimization of benzimidazoles as selective Na<sub>V</sub>1.8 blockers for the treatment of pain
No full text
Polyaromatic Scavenger Reagents (PAHSR): A New Methodology for Rapid Purification in Solution-Phase Combinatorial Synthesis
No full textDiscovery of a Series of Indazole TRPA1 Antagonists
No full textA series
of TRPA1 antagonists is described which has as its core
structure an indazole moiety. The physical properties and <i>in vitro</i> DMPK profiles are discussed. Good <i>in vivo</i> exposure was obtained with several analogs, allowing efficacy to
be assessed in rodent models of inflammatory pain. Two compounds showed
significant activity in these models when administered either systemically
or topically. Protein chimeras were constructed to indicate compounds
from the series bound in the S5 region of the channel, and a computational
docking model was used to propose a binding mode for example compounds
