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John M Keith

Explore the profile of John M Keith including associated specialties, affiliations and a list of published articles. Areas
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Articles 27
Citations 192
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Recent Articles
1.
Keith J, Jones W, Pierce J, Seierstad M, Palmer J, Webb M, et al.
Bioorg Med Chem Lett . 2020 Aug; 30(20):127463. PMID: 32784090
A series of mechanism-based heteroaryl urea fatty acid amide hydrolase (FAAH) inhibitors with fused bicyclic diamine cores is described. In contrast to compounds built around a piperazine core, most of...
2.
Keith J, Tichenor M, Apodaca R, Xiao W, Jones W, Seierstad M, et al.
Bioorg Med Chem Lett . 2016 May; 26(13):3109-3114. PMID: 27189675
The SAR of brain penetration for a series of heteroaryl piperazinyl- and piperadinyl-urea fatty acid amide hydrolase (FAAH) inhibitors is described. Brain/plasma (B/P) ratios ranging from >4:1 to as low...
3.
Blevitt J, Hack M, Herman K, Chang L, Keith J, Mirzadegan T, et al.
J Biol Chem . 2016 Apr; 291(24):12724-12731. PMID: 27129215
5-Lipoxygenase activating protein (FLAP) plays a critical role in the metabolism of arachidonic acid to leukotriene A4, the precursor to the potent pro-inflammatory mediators leukotriene B4 and leukotriene C4 Studies...
4.
Keith J, Jones W, Tichenor M, Liu J, Seierstad M, Palmer J, et al.
ACS Med Chem Lett . 2015 Dec; 6(12):1204-8. PMID: 26713105
The pre-clinical characterization of the aryl piperazinyl urea inhibitor of fatty acid amide hydrolase (FAAH) JNJ-42165279 is described. JNJ-42165279 covalently inactivates the FAAH enzyme, but is highly selective with regard...
5.
Song J, Liu X, Zhu J, Tootoonchi M, Keith J, Meduna S, et al.
J Biomol Screen . 2015 Oct; 21(2):127-35. PMID: 26442913
Leukotrienes (LTs) and related species are proinflammatory lipid mediators derived from arachidonic acid (AA) that have pathological roles in autoimmune and inflammatory conditions, cardiovascular diseases, and cancer. 5-Lipoxygenase activating protein...
6.
Keith J, Apodaca R, Tichenor M, Xiao W, Jones W, Pierce J, et al.
ACS Med Chem Lett . 2014 Jun; 3(10):823-7. PMID: 24900385
A series of aryl piperazinyl ureas that act as covalent inhibitors of fatty acid amide hydrolase (FAAH) is described. A potent and selective (does not inhibit FAAH-2) member of this...
7.
Keith J, Hawryluk N, Apodaca R, Chambers A, Pierce J, Seierstad M, et al.
Bioorg Med Chem Lett . 2014 Feb; 24(5):1280-4. PMID: 24513048
A series of 1-aryl-2-(((6-aryl)pyrimidin-4-yl)amino)ethanols have been found to be competitive inhibitors of fatty acid amide hydrolase (FAAH). One member of this class, JNJ-40413269, was found to have excellent pharmacokinetic properties,...
8.
Keith J, Jones W, Pierce J, Seierstad M, Palmer J, Webb M, et al.
Bioorg Med Chem Lett . 2014 Jan; 24(3):737-41. PMID: 24433863
A series of mechanism based heteroaryl urea fatty acid amide hydrolase (FAAH) inhibitors with spirocyclic diamine cores is described. A potent member of this class, (37), was found to inhibit...
9.
Keith J
J Org Chem . 2012 Dec; 77(24):11313-8. PMID: 23215457
Various pyridine, quinoline, isoquinoline, and pyrimidine N-oxides were converted to their corresponding α-N-aryltriflamidoheteroarenes in good yield by treatment with N-aryltriflimides, both neat and in solution, at temperatures ranging from rt...
10.
Tichenor M, Keith J, Jones W, Pierce J, Merit J, Hawryluk N, et al.
Bioorg Med Chem Lett . 2012 Nov; 22(24):7357-62. PMID: 23141911
The structure-activity relationships for a series of heteroaryl urea inhibitors of fatty acid amide hydrolase (FAAH) are described. Members of this class of inhibitors have been shown to inactivate FAAH...