Discovery of a 4-aryloxy-1H-pyrrolo[3,2-c]pyridine and a 1-aryloxyisoquinoline series of TRPA1 antagonists

A series of TRPA1 antagonists is described having a 4-aryloxy-1H-pyrrolo[3,2-c]pyridine or a 1-aryloxyisoquinoline scaffold. These compounds have high ligand efficiency and favorable physical properties and may thus serve as scaffolds for further optimization.

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Bibliographische Detailangaben
Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2014-07, Vol.24 (14), p.3199-3203
Hauptverfasser:	Hu, Yun-Jin, St.-Onge, Miguel, Laliberté, Sébastien, Vallée, Frédéric, Jin, Shujuan, Bedard, Leanne, Labrecque, Jean, Albert, Jeffrey S.
Format:	Artikel
Sprache:	eng
Schlagworte:	Antagonist Calcium Channels Dose-Response Relationship, Drug Drug Discovery Humans Isoquinolines - chemical synthesis Isoquinolines - chemistry Isoquinolines - pharmacology Ligand gated ion channel Molecular Structure Nerve Tissue Proteins - antagonists & inhibitors Pyridines - chemical synthesis Pyridines - chemistry Pyridines - pharmacology Pyrroles - chemical synthesis Pyrroles - chemistry Pyrroles - pharmacology Structure-Activity Relationship Transient Receptor Potential Channels - antagonists & inhibitors TRPA1 TRPA1 Cation Channel
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Beschreibung
Zusammenfassung:	A series of TRPA1 antagonists is described having a 4-aryloxy-1H-pyrrolo[3,2-c]pyridine or a 1-aryloxyisoquinoline scaffold. These compounds have high ligand efficiency and favorable physical properties and may thus serve as scaffolds for further optimization.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2014.04.045