Scaffold hopping from pyridones to imidazo[1,2-a]pyridines. New positive allosteric modulators of metabotropic glutamate 2 receptor

Bioorganic & Medicinal Chemistry Letters
Gary TresadernAndrés A Trabanco

Abstract

Imidazo[1,2-a]pyridines were identified via their shape and electrostatic similarity as novel positive allosteric modulators of the metabotropic glutamate 2 receptor. The subsequent synthesis and SAR are described. Potent, selective and metabolically stable compounds were found representing a promising avenue for current further studies.

References

May 29, 2003·Current Drug Targets. CNS and Neurological Disorders·Darryle D Schoepp DD, Gerard J Marek
Jun 26, 2003·Neuropsychopharmacology : Official Publication of the American College of Neuropsychopharmacology·Daniel S LorrainLinda J Bristow
May 17, 2007·Current Drug Targets·Max RécasensGérard Barbanel
Jan 1, 2009·Nature Reviews. Drug Discovery·P Jeffrey ConnCraig W Lindsley

❮ Previous
Next ❯

Citations

Feb 23, 2012·Journal of Medicinal Chemistry·Andrés A TrabancoJosé María Cid
Jun 2, 2012·Journal of Medicinal Chemistry·Francois BischoffHarrie J M Gijsen
Mar 24, 2011·Future Medicinal Chemistry·Gary Tresadern, Daniele Bemporad
Nov 22, 2015·British Journal of Pharmacology·Maarten L J DoornbosLaura H Heitman
Mar 5, 2013·Expert Opinion on Therapeutic Patents·Andrés A Trabanco, José María Cid
Aug 5, 2014·Journal of Molecular Graphics & Modelling·Gary TresadernAndrés A Trabanco
Jun 27, 2017·Structure·Laura Pérez-BenitoGary Tresadern
Sep 8, 2012·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Emilie MarieAlain Gueiffier
Mar 23, 2019·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Claudia Llinas Del TorrentGary Tresadern
Mar 19, 2020·ACS Medicinal Chemistry Letters·Ana Isabel de LucasJosé María Cid
Nov 28, 2017·Journal of Chemical Information and Modeling·Gary TresadernGerard J P van Westen

❮ Previous
Next ❯

Related Concepts

Trending Feeds

COVID-19

Coronaviruses encompass a large family of viruses that cause the common cold as well as more serious diseases, such as the ongoing outbreak of coronavirus disease 2019 (COVID-19; formally known as 2019-nCoV). Coronaviruses can spread from animals to humans; symptoms include fever, cough, shortness of breath, and breathing difficulties; in more severe cases, infection can lead to death. This feed covers recent research on COVID-19.

Blastomycosis

Blastomycosis fungal infections spread through inhaling Blastomyces dermatitidis spores. Discover the latest research on blastomycosis fungal infections here.

Nuclear Pore Complex in ALS/FTD

Alterations in nucleocytoplasmic transport, controlled by the nuclear pore complex, may be involved in the pathomechanism underlying multiple neurodegenerative diseases including Amyotrophic Lateral Sclerosis and Frontotemporal Dementia. Here is the latest research on the nuclear pore complex in ALS and FTD.

Applications of Molecular Barcoding

The concept of molecular barcoding is that each original DNA or RNA molecule is attached to a unique sequence barcode. Sequence reads having different barcodes represent different original molecules, while sequence reads having the same barcode are results of PCR duplication from one original molecule. Discover the latest research on molecular barcoding here.

Chronic Fatigue Syndrome

Chronic fatigue syndrome is a disease characterized by unexplained disabling fatigue; the pathology of which is incompletely understood. Discover the latest research on chronic fatigue syndrome here.

Evolution of Pluripotency

Pluripotency refers to the ability of a cell to develop into three primary germ cell layers of the embryo. This feed focuses on the mechanisms that underlie the evolution of pluripotency. Here is the latest research.

Position Effect Variegation

Position Effect Variagation occurs when a gene is inactivated due to its positioning near heterochromatic regions within a chromosome. Discover the latest research on Position Effect Variagation here.

STING Receptor Agonists

Stimulator of IFN genes (STING) are a group of transmembrane proteins that are involved in the induction of type I interferon that is important in the innate immune response. The stimulation of STING has been an active area of research in the treatment of cancer and infectious diseases. Here is the latest research on STING receptor agonists.

Microbicide

Microbicides are products that can be applied to vaginal or rectal mucosal surfaces with the goal of preventing, or at least significantly reducing, the transmission of sexually transmitted infections. Here is the latest research on microbicides.