QSAR modeling of mono-and bis-quaternary ammonium salts that act as antagonists at neuronal nicotinic acetylcholine receptors mediating dopamine release

F Zheng, E Bayram, SP Sumithran, JT Ayers… - Bioorganic & medicinal …, 2006 - Elsevier
Back-propagation artificial neural networks (ANNs) were trained on a dataset of 42 molecules
with quantitative IC 50 values to model structure–activity relationships of mono- and bis-…

bis-Azaaromatic quaternary ammonium analogues: ligands for α4β2* and α7* subtypes of neuronal nicotinic receptors

JT Ayers, LP Dwoskin, AG Deaciuc… - Bioorganic & medicinal …, 2002 - Elsevier
A series of bis-nicotinium, bis-pyridinium, bis-picolinium, bis-quinolinium and bis-isoquinolinium
compounds was evaluated for their binding affinity at nicotinic acetylcholine receptors (…

A preparative scale reduction of alkyl disulfides with tributyl phosphine and water

JT Ayers, SR Anderson - Synthetic communications, 1999 - Taylor & Francis
A series of alkyl disulfides has been shown to be reduced by tributyl phosphine at room
temperature. The resulting thiols were then acylated in the same pot and isolated in good yields. …

Subtype-selective nicotinic receptor antagonists: potential as tobacco use cessation agents

…, SP Sumithran, J Zhu, AG Deaciuc, JT Ayers… - Bioorganic & medicinal …, 2004 - Elsevier
Nn-Alkylpicolinium and N,N′-alkyl-bis-picolinium analogues were assessed in nicotinic
receptor (nAChR) assays. The most potent and subtype-selective analogue, N,N′-dodecyl-bis-…

N, N′-Alkane-diyl-bis-3-picoliniums as nicotinic receptor antagonists: inhibition of nicotine-evoked dopamine release and hyperactivity

…, BM Joyce, PR Lockman, VK Manda, JT Ayers… - … of Pharmacology and …, 2008 - ASPET
The current study evaluated a new series of N,N′-alkane-diyl-bis-3-picolinium (bAPi) analogs
with C 6 –C 12 methylene linkers as nicotinic acetylcholine receptor (nAChR) antagonists…

Nn-Alkylnicotinium analogs, a novel class of nicotinic receptor antagonists: interaction with α4β2* and α7* neuronal nicotinic receptors

LH Wilkins, VP Grinevich, JT Ayers, PA Crooks… - … of Pharmacology and …, 2003 - ASPET
The current study demonstrates thatN-n-alkylnicotinium analogs with increasing n-alkyl
chain lengths from 1 to 12 carbons have varying affinity (K i = 90 nM–20 μM) for S-(−)-[ 3 H]…

Recent developments in neuronal nicotinic acetylcholine receptor antagonists

LP Dwoskin, R Xu, JT Ayers… - Expert Opinion on …, 2000 - Taylor & Francis
Neuronal nicotinic acetylcholine receptors (nAChRs) belong to a superfamily of ligand-gated
ion channel receptors and are distributed extensively throughout the central and peripheral …

The preparation of β-substituted amines from mixtures of epoxide opening products via a common aziridinium ion intermediate

SR Anderson, JT Ayers, KM DeVries, F Ito… - Tetrahedron …, 1999 - Elsevier
Here we describe a one-pot synthesis of a series of β-substituted amines as single enantiomers
from an initial regioisomeric mixture of styrene oxide ring-opening products. We also …

Nn-Alkylnicotinium Analogs, A Novel Class of Nicotinic Receptor Antagonist: Inhibition ofS (−)-Nicotine-Evoked [3H] Dopamine Overflow from Superfused Rat Striatal …

LH Wilkins, A Haubner, JT Ayers, PA Crooks… - … of Pharmacology and …, 2002 - ASPET
The structure of the S(−)-nicotine molecule was modified via N-n-alkylation of the pyridine-N
atom to afford a series ofN-n-alkylnicotinium iodide salts with carbon chain lengths varying …

Development of subtype-selective ligands as antagonists at nicotinic receptors mediating nicotine-evoked dopamine release

PA Crooks, JT Ayers, R Xu, SP Sumithran… - Bioorganic & medicinal …, 2004 - Elsevier
Nn-Alkylation of nicotine converts it from an agonist into an antagonist at neuronal nicotinic
acetylcholine receptor subtypes mediating nicotine-evoked dopamine release. …