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Items: 13

1.

The SAR development of substituted purine derivatives as selective CB2 agonists for the treatment of chronic pain.

Guidetti R, Astles PC, Sanderson AJ, Hollinshead SP, Johnson MP, Chambers MG.

Bioorg Med Chem Lett. 2014 Dec 15;24(24):5572-5575. doi: 10.1016/j.bmcl.2014.11.006. Epub 2014 Nov 7.

PMID:
25466177
2.

Unique pharmacology of heteromeric α7β2 nicotinic acetylcholine receptors expressed in Xenopus laevis oocytes.

Zwart R, Strotton M, Ching J, Astles PC, Sher E.

Eur J Pharmacol. 2014 Mar 5;726:77-86.

PMID:
24485886
3.

Selective cannabinoid receptor type 2 (CB2) agonists: optimization of a series of purines leading to the identification of a clinical candidate for the treatment of osteoarthritic pain.

Hollinshead SP, Tidwell MW, Palmer J, Guidetti R, Sanderson A, Johnson MP, Chambers MG, Oskins J, Stratford R, Astles PC.

J Med Chem. 2013 Jul 25;56(14):5722-33. doi: 10.1021/jm400305d. Epub 2013 Jul 3.

PMID:
23795771
4.

Discovery and optimization of novel purines as potent and selective CB2 agonists.

Hollinshead SP, Astles PC, Chambers MG, Johnson MP, Palmer J, Tidwell MW.

Bioorg Med Chem Lett. 2012 Aug 1;22(15):4962-6. doi: 10.1016/j.bmcl.2012.06.035. Epub 2012 Jun 16.

PMID:
22765893
5.

Total synthesis of (+/-)-alpha-isosparteine, (+/-)-beta-isosparteine, and (+/-)-sparteine from a common tetraoxobispidine intermediate.

Norcross NR, Melbardis JP, Solera MF, Sephton MA, Kilner C, Zakharov LN, Astles PC, Warriner SL, Blakemore PR.

J Org Chem. 2008 Oct 17;73(20):7939-51. doi: 10.1021/jo8013512. Epub 2008 Sep 18.

PMID:
18798673
6.

Species selectivity of a nicotinic acetylcholine receptor agonist is conferred by two adjacent extracellular beta4 amino acids that are implicated in the coupling of binding to channel gating.

Young GT, Broad LM, Zwart R, Astles PC, Bodkin M, Sher E, Millar NS.

Mol Pharmacol. 2007 Feb;71(2):389-97. Epub 2006 Oct 25.

PMID:
17065235
7.

A practical synthesis of (+/-)-alpha-isosparteine from a tetraoxobispidine core.

Blakemore PR, Kilner C, Norcross NR, Astles PC.

Org Lett. 2005 Oct 13;7(21):4721-4.

PMID:
16209519
8.

Recent progress in the development of subtype selective nicotinic acetylcholine receptor ligands.

Astles PC, Baker SR, Boot JR, Broad LM, Dell CP, Keenan M.

Curr Drug Targets CNS Neurol Disord. 2002 Aug;1(4):337-48. Review.

PMID:
12769608
9.

Diamine containing VLA-4 antagonists.

Astles PC, Harris NV, Morley AD.

Bioorg Med Chem. 2001 Aug;9(8):2195-202.

PMID:
11504657
10.

Selective ET(A) antagonists. 5. Discovery and structure-activity relationships of phenoxyphenylacetic acid derivatives.

Astles PC, Brown TJ, Halley F, Handscombe CM, Harris NV, Majid TN, McCarthy C, McLay IM, Morley A, Porter B, Roach AG, Sargent C, Smith C, Walsh RJ.

J Med Chem. 2000 Mar 9;43(5):900-10.

PMID:
10715156
11.

Selective endothelin A receptor antagonists. 4. Discovery and structure-activity relationships of stilbene acid and alcohol derivatives.

Astles PC, Brown TJ, Halley F, Handscombe CM, Harris NV, McCarthy C, McLay IM, Lockey P, Majid T, Porter B, Roach AG, Smith C, Walsh R.

J Med Chem. 1998 Jul 16;41(15):2745-53.

PMID:
9667965
12.

Selective endothelin A receptor antagonists. 3. Discovery and structure-activity relationships of a series of 4-phenoxybutanoic acid derivatives.

Astles PC, Brealey C, Brown TJ, Facchini V, Handscombe C, Harris NV, McCarthy C, McLay IM, Porter B, Roach AG, Sargent C, Smith C, Walsh RJ.

J Med Chem. 1998 Jul 16;41(15):2732-44.

PMID:
9667964
13.

Acyl-CoA:Cholesterol O-acyltransferase (ACAT) inhibitors. 2. 2-(1,3-Dioxan-2-yl)-4,5-diphenyl-1H-imidazoles as potent inhibitors of ACAT.

Astles PC, Ashton MJ, Bridge AW, Harris NV, Hart TW, Parrott DP, Porter B, Riddell D, Smith C, Williams RJ.

J Med Chem. 1996 Mar 29;39(7):1423-32.

PMID:
8691472

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