Allosteric modulation of class A GPCRs: targets, agents, and emerging concepts

EA Wold, J Chen, KA Cunningham… - Journal of medicinal …, 2018 - ACS Publications
G-protein-coupled receptors (GPCRs) have been tractable drug targets for decades with
over one-third of currently marketed drugs targeting GPCRs. Of these, the class A GPCR …

Applications of isosteres of piperazine in the design of biologically active compounds: part 1

NA Meanwell, O Loiseleur - Journal of Agricultural and Food …, 2022 - ACS Publications
Piperazine and homopiperazine are well-studied heterocycles in drug design that have
found gainful application as scaffolds and terminal elements and for enhancing the aqueous …

Cobalt (III)‐Catalyzed Directed C H Coupling with Diazo Compounds: Straightforward Access towards Extended π‐Systems

D Zhao, JH Kim, L Stegemann… - Angewandte Chemie …, 2015 - Wiley Online Library
The first highly efficient and scalable cobalt‐catalyzed directed C H functionalization with
carbene precursors is presented. This methodology provides a modular route towards a new …

Programmable late-stage C− H bond functionalization enabled by integration of enzymes with chemocatalysis

EJ Craven, J Latham, SA Shepherd, I Khan… - Nature Catalysis, 2021 - nature.com
New chemo-and biocatalytic methodology is important for the future sustainable synthesis of
essential molecules. Transition metal catalysis enables the late-stage C− H functionalization …

Fine tuning muscarinic acetylcholine receptor signaling through allostery and bias

ET Van der Westhuizen, KHC Choy, C Valant… - Frontiers in …, 2021 - frontiersin.org
The M1 and M4 muscarinic acetylcholine receptors (mAChRs) are highly pursued drug
targets for neurological diseases, in particular for Alzheimer's disease and schizophrenia …

Allosteric modulation of the M1 muscarinic acetylcholine receptor: improving cognition and a potential treatment for schizophrenia and Alzheimer's disease

BJ Melancon, JC Tarr, JD Panarese, MR Wood… - Drug discovery today, 2013 - Elsevier
Highlights•Dysfunction in glutamatergic and cholinergic signaling in schizophrenia is
discussed.•The advantages of allosteric modulation are discussed.•Activation of the M 1 …

Cognitive enhancers (nootropics). Part 1: drugs interacting with receptors

W Froestl, A Muhs, A Pfeifer - Journal of Alzheimer's disease, 2012 - content.iospress.com
Cognitive enhancers (nootropics) are drugs to treat cognition deficits in patients suffering
from Alzheimer's disease, schizophrenia, stroke, attention deficit hyperactivity disorder, or …

Discovery of the Potent and Selective M1 PAM-Agonist N-[(3R,4S)-3-Hydroxytetrahydro-2H-pyran-4-yl]-5-methyl-4-[4-(1,3-thiazol-4-yl)benzyl]pyridine-2 …

JE Davoren, CW Lee, M Garnsey… - Journal of medicinal …, 2016 - ACS Publications
It is hypothesized that selective muscarinic M1 subtype activation could be a strategy to
provide cognitive benefits to schizophrenia and Alzheimer's disease patients while …

Drug design targeting the muscarinic receptors and the implications in central nervous system disorders

CR Johnson, BD Kangas, EM Jutkiewicz, J Bergman… - Biomedicines, 2022 - mdpi.com
There is substantial evidence that cholinergic system function impairment plays a significant
role in many central nervous system (CNS) disorders. During the past three decades …

Rhodium (III)-catalyzed annulation of pyridinones with alkynes via double C–H activation: a route to functionalized quinolizinones

J Li, Y Yang, Z Wang, B Feng, J You - Organic letters, 2017 - ACS Publications
A Rh (III)-catalyzed oxidative annulation of pyridin-2 (1 H)-ones with alkynes via double C–H
activation to produce highly functionalized 4 H-quinolizin-4-ones is disclosed. This reaction …