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Kevin W Gillman

Explore the profile of Kevin W Gillman including associated specialties, affiliations and a list of published articles. Areas
Snapshot
Articles 11
Citations 141
Followers 0
Related Specialties
Pharmacology
Biochemistry
Chemistry
Top 10 Co-Authors
John E Macor
Joanne J Bronson
Nicholas J Lodge
Yu-Wen Li
Carl D Davis
Amy E Newton
John E Starrett Jr
Donna M Barten
George O Tora
Rick L Pieschl
Published In
J Pharmacol Exp Ther
Bioorg Med Chem Lett
J Labelled Comp Radiopharm
Bioorg Med Chem
Neuropharmacology
Affiliations
Soon will be listed here.
Recent Articles
1.
Nickel-Electrocatalytic Decarboxylative Arylation to Access Quaternary Centers
Laudadio G, Neigenfind P, Peter A, Rubel C, Emmanuel M, Oderinde M, et al.
Angew Chem Int Ed Engl . 2024 Jan; 63(8):e202314617. PMID: 38181042
There is a pressing need, particularly in the field of drug discovery, for general methods that will enable direct coupling of tertiary alkyl fragments to (hetero)aryl halides. Herein a uniquely...
2.
Discovery of Indazoles as Potent, Orally Active Dual Neurokinin 1 Receptor Antagonists and Serotonin Transporter Inhibitors for the Treatment of Depression
Degnan A, Tora G, Huang H, Conlon D, Davis C, Hanumegowda U, et al.
ACS Chem Neurosci . 2016 Oct; 7(12):1635-1640. PMID: 27744678
Combination studies of neurokinin 1 (NK1) receptor antagonists and serotonin-selective reuptake inhibitors (SSRIs) have shown promise in preclinical models of depression. Such a combination may offer important advantages over the...
3.
Biaryls as potent, tunable dual neurokinin 1 receptor antagonists and serotonin transporter inhibitors
Degnan A, Tora G, Han Y, Rajamani R, Bertekap R, Krause R, et al.
Bioorg Med Chem Lett . 2015 Jun; 25(15):3039-43. PMID: 26048800
Depression is a serious illness that affects millions of patients. Current treatments are associated with a number of undesirable side effects. Neurokinin 1 receptor (NK1R) antagonists have recently been shown...
4.
Synthesis of carbon-14 and stable isotope labeled Avagacestat: a novel gamma secretase inhibitor for the treatment of Alzheimer's disease
Burrell R, Easter J, Cassidy M, Gillman K, Olson R, Bonacorsi S
J Labelled Comp Radiopharm . 2014 Sep; 57(10):600-5. PMID: 25196195
Bristol-Myers Squibb and others are developing drugs that target novel mechanisms to combat Alzheimer's disease. γ-Secretase inhibitors are one class of potential therapies that have received considerable attention. (R)-2-(4-Chloro-N-(2-fluoro-4-(1,2,4-oxadiazol-3-yl)benzyl)phenylsulfonamido)-5,5,5-trifluoropentanamide (Avagacestat)...
5.
Discovery and Evaluation of BMS-708163, a Potent, Selective and Orally Bioavailable γ-Secretase Inhibitor
Gillman K, Starrett Jr J, Parker M, Xie K, Bronson J, Marcin L, et al.
ACS Med Chem Lett . 2014 Jun; 1(3):120-4. PMID: 24900185
During the course of our research efforts to develop a potent and selective γ-secretase inhibitor for the treatment of Alzheimer's disease, we investigated a series of carboxamide-substituted sulfonamides. Optimization based...
6.
NK1 receptor antagonism lowers occupancy requirement for antidepressant-like effects of SSRIs in the gerbil forced swim test
Lelas S, Li Y, Wallace-Boone T, Taber M, Newton A, Pieschl R, et al.
Neuropharmacology . 2013 Jun; 73:232-40. PMID: 23770339
The known interactions between the serotonergic and neurokinin systems suggest that serotonin reuptake inhibitor (SSRIs) efficacy may be improved by neurokinin-1 receptor (NK1R) antagonism. In the current studies combination of...
7.
Pharmacodynamics of selective inhibition of γ-secretase by avagacestat
Albright C, Dockens R, Meredith Jr J, Olson R, Slemmon R, Lentz K, et al.
J Pharmacol Exp Ther . 2013 Jan; 344(3):686-95. PMID: 23275065
A hallmark of Alzheimer's disease (AD) pathology is the accumulation of brain amyloid β-peptide (Aβ), generated by γ-secretase-mediated cleavage of the amyloid precursor protein (APP). Therefore, γ-secretase inhibitors (GSIs) may...
8.
Design, optimization, and in vivo evaluation of a series of pyridine derivatives with dual NK1 antagonism and SERT inhibition for the treatment of depression
Gillman K, Parker M, Silva M, Degnan A, Tora G, Lodge N, et al.
Bioorg Med Chem Lett . 2012 Dec; 23(2):407-11. PMID: 23253443
A series of substituted pyridines, ether linked to a phenylpiperidine core were optimized for dual NK(1)/SERT affinity. Optimization based on NK(1)/SERT binding affinities, and minimization of off-target ion channel activity...
9.
Donepezil primarily attenuates scopolamine-induced deficits in psychomotor function, with moderate effects on simple conditioning and attention, and small effects on working memory and spatial mapping
Lindner M, Hogan J, Hodges Jr D, Orie A, Chen P, Corsa J, et al.
Psychopharmacology (Berl) . 2006 Sep; 188(4):629-40. PMID: 17004085
Rationale: Alzheimer's dementia (AD) patients have profound deficits in cognitive and social functions, mediated in part by a decline in cholinergic function. Acetylcholinesterase inhibitors (AChEI) are the most commonly prescribed...
10.
Synthesis and evaluation of 5,5-diphenylimidazolones as potent human neuropeptide Y5 receptor antagonists
Gillman K, Higgins M, Poindexter G, Browning M, Clarke W, Flowers S, et al.
Bioorg Med Chem . 2006 May; 14(16):5517-26. PMID: 16697206
A series of novel 5,5-diphenylimidazolones was synthesized and evaluated for activity against the human neuropeptide Y5 receptor. The 3-pyridyl analog 46 demonstrated an IC(50) of 8.3 nM with a favorable...