William H Bunnelle
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Explore the profile of William H Bunnelle including associated specialties, affiliations and a list of published articles.
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27
Citations
380
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Recent Articles
11.
Bunnelle W, Tietje K, Frost J, Peters D, Ji J, Li T, et al.
J Med Chem
. 2009 Jun;
52(14):4126-41.
PMID: 19552432
A series of 5-(pyridine-3-yl)octahydropyrrolo[3,4-c]pyrroles have been prepared that exhibit high affinity to alpha4beta2 and/or alpha7 nicotinic acetylcholine receptors (nAChRs). Simple substitution patterns have been identified that allow construction of ligands...
12.
Faghih R, Gopalakrishnan S, Gronlien J, Malysz J, Briggs C, Wetterstrand C, et al.
J Med Chem
. 2009 May;
52(10):3377-84.
PMID: 19419141
The discovery of a series of pyrrole-sulfonamides as positive allosteric modulators (PAM) of alpha7 nAChRs is described. Optimization of this series led to the identification of 19 (A-867744), a novel...
13.
Malysz J, Gronlien J, Anderson D, Hakerud M, Thorin-Hagene K, Ween H, et al.
J Pharmacol Exp Ther
. 2009 Apr;
330(1):257-67.
PMID: 19389923
Targeting alpha7 neuronal acetylcholine receptors (nAChRs) with selective agonists and positive allosteric modulators (PAMs) is considered a therapeutic approach for managing cognitive deficits in schizophrenia and Alzheimer's disease. In this...
14.
Sippy K, Anderson D, Bunnelle W, Hutchins C, Schrimpf M
Bioorg Med Chem Lett
. 2009 Feb;
19(6):1682-5.
PMID: 19232492
Several N-pyridin-3-yl spirobicyclic diamines, designed as conformationally restricted analogs of tebanicline (ABT-594), were synthesized as novel ligands for nicotinic acetylcholine receptors (nAChR). The spirocyclic compounds exhibited weaker binding affinity, than...
15.
Tietje K, Anderson D, Bitner R, Blomme E, Brackemeyer P, Briggs C, et al.
CNS Neurosci Ther
. 2008 May;
14(1):65-82.
PMID: 18482100
Among the diverse sets of nicotinic acetylcholine receptors (nAChRs), the alpha7 subtype is highly expressed in the hippocampus and cortex and is thought to play important roles in a variety...
16.
Ji J, Schrimpf M, Sippy K, Bunnelle W, Li T, Anderson D, et al.
J Med Chem
. 2007 Oct;
50(22):5493-508.
PMID: 17929796
A series of novel, potent neuronal nicotinic acetylcholine receptor (nAChR) ligands derived from 3,6-diazabicyclo[3.2.0]heptane have been synthesized and evaluated for binding affinity and agonist activity at the alpha4beta2 nAChR subtype....
17.
Bitner R, Bunnelle W, Anderson D, Briggs C, Buccafusco J, Curzon P, et al.
J Neurosci
. 2007 Sep;
27(39):10578-87.
PMID: 17898229
The alpha7 nicotinic acetylcholine receptor (nAChR) plays an important role in cognitive processes and may represent a drug target for treating cognitive deficits in neurodegenerative and psychiatric disorders. In the...
18.
Ji J, Bunnelle W, Anderson D, Faltynek C, Dyhring T, Ahring P, et al.
Biochem Pharmacol
. 2007 Sep;
74(8):1253-62.
PMID: 17854775
5-[(1R,5S)-3,6-Diazabicyclo[3.2.0]heptan-6-yl]nicotinonitrile (A-366833) is a novel nicotinic acetylcholine receptor (nAChR) ligand that binds to the agonist-binding site ([3H]-cytisine) with Ki value of 3.1 nM and exhibits agonist selectivity at alpha4beta2 nAChR...
19.
Bunnelle W, Daanen J, Ryther K, Schrimpf M, Dart M, Gelain A, et al.
J Med Chem
. 2007 Jun;
50(15):3627-44.
PMID: 17585748
A series of exceptionally potent agonists at neuronal nicotinic acetylcholine receptors (nAChRs) has been investigated. Several N-(3-pyridinyl) derivatives of bridged bicyclic diamines exhibit double-digit-picomolar binding affinities for the alpha 4...
20.
Frost J, Bunnelle W, Tietje K, Anderson D, Rueter L, Curzon P, et al.
J Med Chem
. 2006 Dec;
49(26):7843-53.
PMID: 17181167
A series of potent neuronal nicotinic acetylcholine receptor (nAChR) ligands based on a 3,8-diazabicyclo[4.2.0]octane core have been synthesized and evaluated for affinity and agonist efficacy at the human high affinity...