Discovery and in vitro and in vivo profiles of 4-fluoro-N-[4-[6-(isopropylamino) pyrimidin-4-yl]-1, 3-thiazol-2-yl]-N-methylbenzamide as novel class of an orally active …

A Satoh, Y Nagatomi, Y Hirata, S Ito, G Suzuki… - Bioorganic & medicinal …, 2009 - Elsevier
We identified 4-fluoro-N-[4-[6-(isopropylamino) pyrimidin-4-yl]-1, 3-thiazol-2-yl]-N-
methylbenzamide 27 as a potent mGluR1 antagonist. The compound possessed excellent …

Recent Advances in the Medicinal Chemistry of the Metabotropic Glutamate Receptor 1 (mGlu1)

DR Owen - ACS Chemical Neuroscience, 2011 - ACS Publications
This Review summarizes the medicinal chemistry found in publications on both orthosteric
and allosteric modulators of the metabotropic glutamate receptor 1 (mGlu1) from 2005 to the …

A novel class of succinimide-derived negative allosteric modulators of metabotropic glutamate receptor subtype 1 provides insight into a disconnect in activity between …

HP Cho, DW Engers, DF Venable… - ACS Chemical …, 2014 - ACS Publications
Recent progress in the discovery of mGlu1 allosteric modulators has suggested the
modulation of mGlu1 could offer possible treatment for a number of central nervous system …

One-pot etherification of purine nucleosides and pyrimidines

HP Kokatla, MK Lakshman - Organic letters, 2010 - ACS Publications
A one-pot synthesis of ethers derived from inosine, guanosine, 2′-deoxyguanosine, and
pyrimidinones is described. Exposure of the heterocycle to 1 H-benzotriazol-1-yloxy-tris …

Metabotropic glutamate receptors in GtoPdb v. 2023.1

F Acher, G Battaglia, H Bräuner-Osborne… - IUPHAR/BPS Guide …, 2023 - journals.ed.ac.uk
Metabotropic glutamate (mGlu) receptors (nomenclature as agreed by the NC-IUPHAR
Subcommittee on Metabotropic Glutamate Receptors [351]) are a family of G protein …

Novel scaffold identification of mg lu1 receptor negative allosteric modulators using a hierarchical virtual screening approach

JW Jang, NC Cho, SJ Min, YS Cho… - Chemical biology & …, 2016 - Wiley Online Library
Metabotropic glutamate receptor 1 (mG luR1) is considered as an attractive drug target for
neuropathic pain treatments. The hierarchical virtual screening approach for identifying …

N-Acyl-N′-arylpiperazines as negative allosteric modulators of mGlu1: Identification of VU0469650, a potent and selective tool compound with CNS exposure in rats

KM Lovell, AS Felts, AL Rodriguez, DF Venable… - Bioorganic & medicinal …, 2013 - Elsevier
Development of SAR in an N-acyl-N′-arylpiperazine series of negative allosteric
modulators of mGlu1 using a functional cell-based assay is described in this Letter …

Discovery of novel mGluR1 antagonists: a multistep virtual screening approach based on an SVM model and a pharmacophore hypothesis significantly increases the …

GB Li, LL Yang, S Feng, JP Zhou, Q Huang… - Bioorganic & medicinal …, 2011 - Elsevier
Development of glutamate non-competitive antagonists of mGluR1 (Metabotropic glutamate
receptor subtype 1) has increasingly attracted much attention in recent years due to their …

A Novel Synthesis of Quinazolines by Cyclization of 1‐(2‐Isocyanophenyl) alkylideneamines Generated by the Treatment of 2‐(1‐Azidoalkyl) phenyl Isocyanides with …

K Ezaki, K Kobayashi - Helvetica Chimica Acta, 2014 - Wiley Online Library
A new and efficient method for the synthesis of quinazolines has been developed. Thus, N‐
[2‐(1‐azidoalkyl) phenyl] formamides 1 are dehydrated with POCl3 to give the …

Novel thienopyrimidinones as mGluR1 antagonists

Y Kim, J Kim, S Kim, Y Ki, SH Seo, J Tae, MK Ko… - European Journal of …, 2014 - Elsevier
There has been much attention to discover mGluR1 antagonists for treating various central
nervous system diseases such as seizures and neuropathic pain. Thienopyrimidinone …