2-Methyl-3-furanyl-4H-1,2,4-triazol-3-ylthioamides: a new class of selective orexin 2 antagonists

Fabrizio Micheli; Marinella Antolini; Romano Di Fabio; Annalisa Pellacani; Alfonso Pozzan

doi:10.1016/j.bmcl.2010.09.090

2-Methyl-3-furanyl-4H-1,2,4-triazol-3-ylthioamides: a new class of selective orexin 2 antagonists

Bioorg Med Chem Lett. 2010 Nov 15;20(22):6405-7. doi: 10.1016/j.bmcl.2010.09.090. Epub 2010 Sep 19.

Authors

Fabrizio Micheli¹, Marinella Antolini, Romano Di Fabio, Annalisa Pellacani, Alfonso Pozzan

Affiliation

¹ Neurosciences Centre of Excellence, GlaxoSmithKline Medicines Research Centre, Via Fleming 4, 37135 Verona, Italy. fabrizio.micheli@aptuit.com

PMID: 20933413
DOI: 10.1016/j.bmcl.2010.09.090

Abstract

A new class of selective orexin 2 antagonist was identified among commercial products. Initial SAR was obtained using commercial derivatives only prior to starting ad hoc medicinal chemistry activities.

MeSH terms

Animals
Humans
Models, Molecular
Orexin Receptors
Rats
Receptors, G-Protein-Coupled / antagonists & inhibitors*
Receptors, Neuropeptide / antagonists & inhibitors*
Structure-Activity Relationship
Triazoles / chemistry
Triazoles / pharmacology*

Substances

Orexin Receptors
Receptors, G-Protein-Coupled
Receptors, Neuropeptide
Triazoles