Jon G A Steadman
Overview
Explore the profile of Jon G A Steadman including associated specialties, affiliations and a list of published articles.
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Articles
7
Citations
41
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Recent Articles
1.
Wilson D, Apps J, Bailey N, Bamford M, Beresford I, Brackenborough K, et al.
Bioorg Med Chem Lett
. 2013 Nov;
23(24):6890-6.
PMID: 24269482
This Letter describes the discovery of GSK189254 and GSK239512 that were progressed as clinical candidates to explore the potential of H3 receptor antagonists as novel therapies for the treatment of...
2.
Wilson D, Apps J, Bailey N, Bamford M, Beresford I, Briggs M, et al.
Bioorg Med Chem Lett
. 2013 Oct;
23(24):6897-901.
PMID: 24161834
This Letter describes the discovery of a novel series of H3 receptor antagonists. The initial medicinal chemistry strategy focused on deconstructing and simplifying an early screening hit which rapidly led...
3.
Abberley L, Bebius A, Beswick P, Billinton A, Collis K, Dean D, et al.
Bioorg Med Chem Lett
. 2010 Oct;
20(22):6370-4.
PMID: 20934331
A backup molecule to compound 2 was sought by targeting the most likely metabolically vulnerable site in this molecule. Compound 18 was subsequently identified as a potent P2X(7) antagonist with...
4.
Abdi M, Beswick P, Billinton A, Chambers L, Charlton A, Collins S, et al.
Bioorg Med Chem Lett
. 2010 Aug;
20(17):5080-4.
PMID: 20673717
A computational lead-hopping exercise identified compound 4 as a structurally distinct P2X(7) receptor antagonist. Structure-activity relationships (SAR) of a series of pyroglutamic acid amide analogues of 4 were investigated and...
5.
Witherington J, Abberley L, Bellenie B, Boatman R, Collis K, Dean D, et al.
Bioorg Med Chem Lett
. 2009 Jan;
19(3):684-7.
PMID: 19128969
As part of an on-going lead optimisation effort, a cross screening exercise identified an aryl sulphonyl amide hit that was optimised to afford a highly potent series of ghrelin receptor...
6.
Takle A, Bamford M, Davies S, Davis R, Dean D, Gaiba A, et al.
Bioorg Med Chem Lett
. 2008 Jul;
18(15):4373-6.
PMID: 18621524
Modification of the potent imidazole-based B-Raf inhibitor SB-590885 resulted in the identification of a series of furan-based derivatives with enhanced CNS penetration. One such compound, SB-699393 (17), was examined in...
7.
Witherington J, Abberley L, Briggs M, Collis K, Dean D, Gaiba A, et al.
Bioorg Med Chem Lett
. 2008 Mar;
18(6):2203-5.
PMID: 18316188
A series of small molecule orally bioavailable ghrelin receptor agonists have been identified through systematic optimisation of a high throughput screening hit.