Allosteric GABAA Receptor Modulators—A Review on the Most Recent Heterocyclic Chemotypes and Their Synthetic Accessibility
BA Vega Alanis, MT Iorio, LL Silva, K Bampali, M Ernst… - Molecules, 2020 - mdpi.com
… This review focuses on the synthetic accessibility and potential for library synthesis of … Within
this review, heterocyclic compounds acting as GABA A receptor modulators will be revised. …
this review, heterocyclic compounds acting as GABA A receptor modulators will be revised. …
Design and Identification of a Novel, Functionally Subtype Selective GABAA Positive Allosteric Modulator (PF-06372865)
RM Owen, D Blakemore, L Cao, N Flanagan, R Fish… - 2019 - ACS Publications
… selectivity exists within a given chemotype, generally it is quite “… a range of different heterocyclic
cores decorated with … ; Kooy, RF The complexity of the GABAA receptor shapes unique …
cores decorated with … ; Kooy, RF The complexity of the GABAA receptor shapes unique …
The Allosteric Modulation of the GABAB Receptor: A Medicinal Chemistry Perspective
C Mugnaini, F Corelli - GABAB receptor, 2016 - Springer
… by a five-membered heterocyclic scaffold functionalized with amide … structural changes of a
given allosteric chemotype. Thus, during … Nature Reviews Drug Discovery, 13, 692–708 and …
given allosteric chemotype. Thus, during … Nature Reviews Drug Discovery, 13, 692–708 and …
Subtype Selective γ-Aminobutyric Acid Type A Receptor (GABAAR) Modulators Acting at the Benzodiazepine Binding Site: An Update
… (PAMs) and α5-GABA A R negative allosteric modulators (… heterocyclic cores (series 1–3,
Figure 4). The imidazopyridazine series (series 2) was selected as the preferred chemotype …
Figure 4). The imidazopyridazine series (series 2) was selected as the preferred chemotype …
Development of 1, 3-thiazole analogues of imidazopyridines as potent positive allosteric modulators of GABAA receptors
TA Tikhonova, IV Rassokhina, EA Kondrakhin… - Bioorganic …, 2020 - Elsevier
… Most chemotypes comprise positive allosteric modulators (… we report the results of our study
on a new series of GABA A R … by sulfur-containing heterocycles was successfully used for the …
on a new series of GABA A R … by sulfur-containing heterocycles was successfully used for the …
Negative allosteric modulators of group II metabotropic glutamate receptors: A patent review (2015–present)
AM Qunies, KA Emmitte - Expert Opinion on Therapeutic Patents, 2021 - Taylor & Francis
… [1,5-a]pyrazinone chemotype which was consistently … chemotypes discussed in this review.
For instance, 20 of the 21 patent applications centered on scaffolds with a fused heterocyclic …
For instance, 20 of the 21 patent applications centered on scaffolds with a fused heterocyclic …
mGlu5 negative allosteric modulators: a patent review (2013 - 2016)
KA Emmitte - Expert opinion on therapeutic patents, 2017 - Taylor & Francis
… compounds from within the broad disubstituted alkyne chemotype. An application from Merz
describes a series of heterocyclic analogs where one of the groups bound to the alkyne is a …
describes a series of heterocyclic analogs where one of the groups bound to the alkyne is a …
Drug development in channelopathies: Allosteric modulation of ligand-gated and voltage-gated ion channels
Y Zhang, K Wang, Z Yu - Journal of medicinal chemistry, 2020 - ACS Publications
… review highlights the discovery of representative allosteric … serious side effects, several
chemotypes of AMPAR NAMs have been … of allosteric modulators targeting GABA A receptors. …
chemotypes of AMPAR NAMs have been … of allosteric modulators targeting GABA A receptors. …
GABAA receptors: structure, function, pharmacology, and related disorders
… Accordingly, this review aims to summarize the current … of GABA A Rs, as well as shedding
light on the most common … , silent allosteric modulators (SAM) are a class of GABA A R …
light on the most common … , silent allosteric modulators (SAM) are a class of GABA A R …
Recent advances in the medicinal chemistry of group II and group III mGlu receptors
C Jin, S Ma - MedChemComm, 2017 - pubs.rsc.org
… , but also the group II and group III allosteric modulators and … the exploration of 6-substituted
chemotypes, with an EC 50 … on a five-membered heterocyclic group and found sulfone …
chemotypes, with an EC 50 … on a five-membered heterocyclic group and found sulfone …