Stephen A Thomson
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Explore the profile of Stephen A Thomson including associated specialties, affiliations and a list of published articles.
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17
Citations
118
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Recent Articles
1.
Schulte C, Deaton D, Diaz E, Do Y, Gampe R, Guss J, et al.
Bioorg Med Chem Lett
. 2021 May;
47:128113.
PMID: 33991628
Through an internal virtual screen at GlaxoSmithKline a distinct class of 2-phenylimidazo[1,2-a]pyridine-6-carboxamide H-PGDS inhibitors were discovered. Careful evaluation of crystal structures and SAR led to a novel, potent, and orally...
2.
Cadilla R, Deaton D, Do Y, Elkins P, Ennulat D, Guss J, et al.
Bioorg Med Chem
. 2020 Oct;
28(23):115791.
PMID: 33059303
GlaxoSmithKline and Astex Pharmaceuticals recently disclosed the discovery of the potent H-PGDS inhibitor GSK2894631A 1a (IC = 9.9 nM) as part of a fragment-based drug discovery collaboration with Astex Pharmaceuticals....
3.
Deaton D, Do Y, Holt J, Jeune M, Kramer H, Larkin A, et al.
Bioorg Med Chem
. 2019 Mar;
27(8):1456-1478.
PMID: 30858025
With the goal of discovering more selective anti-inflammatory drugs, than COX inhibitors, to attenuate prostaglandin signaling, a fragment-based screen of hematopoietic prostaglandin D synthase was performed. The 76 crystallographic hits...
4.
Haffner C, Thomson S, Guo Y, Petrov K, Larkin A, Banker P, et al.
Bioorg Med Chem Lett
. 2010 Oct;
20(23):6989-92.
PMID: 20974533
We report the synthesis and in vitro activity of a series of novel substituted N-{3-[(1,1-dioxido-1,2-benzothiazol-3-yl)(phenyl)amino]propyl}benzamide analogs. These analogs showed potent inhibitory activity against Kv1.3. Several demonstrated similar potency to the...
5.
Haffner C, Thomson S, Guo Y, Schaller L, Boggs S, Dickerson S, et al.
Bioorg Med Chem Lett
. 2010 Oct;
20(23):6983-8.
PMID: 20971642
We report the synthesis and in vitro activity of a series of novel N-{3-[(1,1-dioxido-1,2-benzothiazol-3-yl)(phenyl)amino]propyl}benzamide analogs. These analogs showed potent inhibitory activity against Kv1.3. Several compounds, including compound 8b, showed similar...
6.
Thomson S, Banker P, Bickett D, Boucheron J, Carter H, Clancy D, et al.
Bioorg Med Chem Lett
. 2009 Jan;
19(4):1177-82.
PMID: 19138846
Key binding interactions of the anthranilimide based glycogen phosphorylase a (GPa) inhibitor 2 from X-ray crystallography studies are described. This series of compounds bind to the AMP site of GP....
7.
Sparks S, Banker P, Bickett D, Clancy D, Dickerson S, Garrido D, et al.
Bioorg Med Chem Lett
. 2008 Dec;
19(3):981-5.
PMID: 19095443
Optimization of the amino acid residue of a series of anthranilimide-based glycogen phosphorylase inhibitors is described leading to the identification of serine and threonine ether analogs. t-Butylthreonine analog 20 displayed...
8.
Sparks S, Banker P, Bickett D, Carter H, Clancy D, Dickerson S, et al.
Bioorg Med Chem Lett
. 2008 Dec;
19(3):976-80.
PMID: 19095442
Optimization of the amino acid residue within a series of anthranilimide-based glycogen phosphorylase inhibitors is described. These studies culminated in the identification of anthranilimides 16 and 22 which displayed potent...
9.
Evans K, Li Y, Coppo F, Graybill T, Cichy-Knight M, Patel M, et al.
Bioorg Med Chem Lett
. 2008 Jun;
18(14):4068-71.
PMID: 18554908
A series of amino acid anthranilamide derivatives identified from a high-throughput screening campaign as novel, potent, and glucose-sensitive inhibitors of human liver glycogen phosphorylase a are described. A solid-phase synthesis...
10.
Li Y, Coppo F, Evans K, Graybill T, Patel M, Gale J, et al.
Bioorg Med Chem Lett
. 2006 Sep;
16(22):5892-6.
PMID: 16942879
A series of 3-phenyl-2-propenamides discovered from a high-throughput screening campaign as novel, potent, glucose-sensitive inhibitors of human liver glycogen phosphorylase a is described. A solid-phase synthesis on DMHB resin was...