John M Keith
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Explore the profile of John M Keith including associated specialties, affiliations and a list of published articles.
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27
Citations
192
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Recent Articles
11.
Letavic M, Aluisio L, Atack J, Bonaventure P, Carruthers N, Dugovic C, et al.
Bioorg Med Chem Lett
. 2010 Jun;
20(14):4210-4.
PMID: 20561786
The pre-clinical characterization of novel aryloxypyridine amides that are histamine H(3) receptor antagonists is described. These compounds are high affinity histamine H(3) ligands that penetrate the CNS and occupy the...
12.
Keith J
J Org Chem
. 2010 Mar;
75(8):2722-5.
PMID: 20297806
Pyridine, quinoline, isoquinoline, azaindole, and pyrimidine N-oxides were converted to their alpha-triazole and alpha-diazole derivatives by treatment with the corresponding p-toluenesulfonylazoles and Hunig's base at elevated temperatures.
13.
Karbarz M, Luo L, Chang L, Tham C, Palmer J, Wilson S, et al.
Anesth Analg
. 2008 Dec;
108(1):316-29.
PMID: 19095868
Fatty acid amide hydrolase (FAAH) is an integral membrane enzyme within the amidase-signature family. It catalyzes the hydrolysis of several endogenous biologically active lipids, including anandamide (arachidonoyl ethanolamide), oleoyl ethanolamide,...
14.
Letavic M, Keith J, Ly K, Bonaventure P, Feinstein M, Lord B, et al.
Bioorg Med Chem Lett
. 2008 Oct;
18(21):5796-9.
PMID: 18922693
The synthesis and biological activity of a new series of 2-aryloxymethylmorpholine histamine H(3) antagonists is described. The new compounds are high affinity histamine H(3) ligands that penetrate the CNS and...
15.
Keith J, Apodaca R, Xiao W, Seierstad M, Pattabiraman K, Wu J, et al.
Bioorg Med Chem Lett
. 2008 Aug;
18(17):4838-43.
PMID: 18693015
A series of thiadiazolopiperazinyl aryl urea fatty acid amide hydrolase (FAAH) inhibitors is described. The molecules were found to inhibit the enzyme by acting as mechanism-based substrates, forming a covalent...
16.
Bembenek S, Keith J, Letavic M, Apodaca R, Barbier A, Dvorak L, et al.
Bioorg Med Chem
. 2008 Feb;
16(6):2968-73.
PMID: 18249544
Currently, the only clinically effective treatment for Alzheimer's disease (AD) is the use of acetylcholinesterase (AChE) inhibitors. These inhibitors have limited efficacy in that they only treat the symptoms and...
17.
Keith J
J Org Chem
. 2007 Dec;
73(1):327-30.
PMID: 18067315
Various pyridine-, quinoline-, isoquinoline-, and pyrimidine-N-oxides were converted to their corresponding alpha-imidazoloheteroarenes in good yield by treatment with sulfuryl diimidazole in nonpolar solvents at elevated temperatures.
18.
Ly K, Letavic M, Keith J, Miller J, Stocking E, Barbier A, et al.
Bioorg Med Chem Lett
. 2007 Dec;
18(1):39-43.
PMID: 18060777
The synthesis and biological activity of a new series of piperazine and diazepane amides is described. The new compounds are high affinity histamine H3 ligands and serotonin reuptake inhibitors.
19.
Keith J, Barbier A, Wilson S, Miller K, Boggs J, Fraser I, et al.
Bioorg Med Chem Lett
. 2007 Sep;
17(19):5325-9.
PMID: 17765543
A series of tetrahydroisoquinolines acting as dual serotonin transporter inhibitor/histamine H(3) antagonists is described. The introduction of polar aromatic spacers as part of the histamine H(3) pharmacophore was explored. A...
20.
Keith J, Gomez L, Barbier A, Wilson S, Boggs J, Lord B, et al.
Bioorg Med Chem Lett
. 2007 Jun;
17(15):4374-7.
PMID: 17583504
A series of novel and potent 6-heteroaryl-pyrrolidino-tetrahydroisoquinolines with dual histamine H(3) antagonist/serotonin transporter inhibitor activity is described. In vitro and in vivo data are discussed.