Robert J Gleave
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Explore the profile of Robert J Gleave including associated specialties, affiliations and a list of published articles.
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Recent Articles
1.
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...
2.
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...
3.
Gleave R, Walter D, Beswick P, Fonfria E, Michel A, Roman S, et al.
Bioorg Med Chem Lett
. 2010 Jul;
20(16):4951-4.
PMID: 20634071
A series of analogues of the pyrazole lead 1 were synthesized in which the heterocyclic core was replaced with an imidazole. A number of potent antagonists were identified and structure-activity...
4.
Beswick P, Billinton A, Chambers L, Dean D, Fonfria E, Gleave R, et al.
Bioorg Med Chem Lett
. 2010 Jun;
20(15):4653-6.
PMID: 20579878
Structure-activity relationships (SAR) of analogues of lead compound 1 were investigated and compound 16 was selected for further study in animal models of pain. Compound 16 was shown to be...
5.
Chambers L, Stevens A, Moses A, Michel A, Walter D, Davies D, et al.
Bioorg Med Chem Lett
. 2010 Apr;
20(10):3161-4.
PMID: 20399651
High-throughput screening identified compound 1 as a potent P2X(7) receptor antagonist suitable for lead optimisation. Structure-activity relationships (SAR) of a series of (1H-pyrazol-4-yl)acetamides were investigated and compound 32 was identified...
6.
Gleave R, Beswick P, Brown A, Giblin G, Goldsmith P, Haslam C, et al.
Bioorg Med Chem Lett
. 2009 Dec;
20(2):465-8.
PMID: 20005703
A series of 3-amino-6-aryl-pyridazines have been identified as CB(2) agonists with high efficacy and selectivity against the CB(1) receptor. Details of the investigation of structure-activity relationships (SAR) are disclosed, which...
7.
Gleave R, Beswick P, Brown A, Giblin G, Haslam C, Livermore D, et al.
Bioorg Med Chem Lett
. 2009 Oct;
19(23):6578-81.
PMID: 19864133
2-Amino-5-aryl-pyridines, exemplified by compound 1, had been identified as a synthetically tractable series of CB(2) agonists from a high-throughput screen of the GlaxoSmithKline compound collection. Described herein are the results...
8.
Beswick P, Blackaby A, Bountra C, Brown T, Browning K, Campbell I, et al.
Bioorg Med Chem Lett
. 2009 Jun;
19(15):4509-14.
PMID: 19523822
Many years of work have been invested in the identification of potent and selective COX-2 inhibitors for the treatment of chronic inflammatory pain. One issue faced by workers is the...
9.
Swarbrick M, Beswick P, Gleave R, Green R, Bingham S, Bountra C, et al.
Bioorg Med Chem Lett
. 2009 Jun;
19(15):4504-8.
PMID: 19520573
A novel series of [4-[4-(methylsulfonyl)phenyl]-6-(trifluoromethyl)-2-pyrimidine-based cyclooxygenase-2 (COX-2) inhibitors, which have a different arrangement of substituents compared to the more common 1,2-diarylheterocycle based molecules, have been discovered. For example, 2-(butyloxy)-4-[4-(methylsulfonyl)phenyl]-6-(trifluoromethyl)pyrimidine (47),...
10.
Hall A, Atkinson S, Brown S, Chessell I, Chowdhury A, Clayton N, et al.
Bioorg Med Chem Lett
. 2006 May;
16(14):3657-62.
PMID: 16697196
The preliminary SAR of a series of novel 1,5-biaryl pyrrole EP1 receptor antagonists derived from compound 1 is described. Replacement of the benzyl group of 1 with isosteric groups was...