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 …
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 …
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 …
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 …
essential molecules. Transition metal catalysis enables the late-stage C− H functionalization …
Fine tuning muscarinic acetylcholine receptor signaling through allostery and bias
The M1 and M4 muscarinic acetylcholine receptors (mAChRs) are highly pursued drug
targets for neurological diseases, in particular for Alzheimer's disease and schizophrenia …
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 …
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 …
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 …
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
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 …
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 …
activation to produce highly functionalized 4 H-quinolizin-4-ones is disclosed. This reaction …