Bryan J Branstetter
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Explore the profile of Bryan J Branstetter including associated specialties, affiliations and a list of published articles.
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5
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13
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Recent Articles
1.
Rech J, Bhattacharya A, Branstetter B, Love C, Leenaerts J, Cooymans L, et al.
Bioorg Med Chem Lett
. 2016 Sep;
26(19):4781-4784.
PMID: 27595421
The synthesis, SAR and preclinical characterization of a series of 6-chloro-N-(2-(4,4-difluoropiperidin-1-yl)-2-(2-(trifluoromethyl)pyrimidin-5-yl)ethyl)quinoline-5-carboxamide based P2X7 antagonists is described herein. The lead compounds are potent inhibitors in Ca(2+) flux and whole blood IL-1β...
2.
Maher M, Bhattacharya A, Ao H, Swanson N, Wu N, Freedman J, et al.
Eur J Pharmacol
. 2011 May;
663(1-3):40-50.
PMID: 21575625
As an integrator of multiple nociceptive and/or inflammatory stimuli, TRPV1 is an attractive therapeutic target for the treatment of various painful disorders. Several TRPV1 antagonists have been advanced into clinical...
3.
Discovery and synthesis of 6,7,8,9-tetrahydro-5H-pyrimido-[4,5-d]azepines as novel TRPV1 antagonists
Hawryluk N, Merit J, Lebsack A, Branstetter B, Hack M, Swanson N, et al.
Bioorg Med Chem Lett
. 2010 Oct;
20(23):7137-41.
PMID: 20947352
Utilization of a tetrahydro-pyrimdoazepine core as a bioisosteric replacement for a piperazine-urea resulted in the discovery a novel series of potent antagonists of TRPV1. The tetrahydro-pyrimdoazepines have been identified as...
4.
Lebsack A, Rech J, Branstetter B, Hawryluk N, Merit J, Allison B, et al.
Bioorg Med Chem Lett
. 2010 Oct;
20(23):7142-6.
PMID: 20932750
Based upon a previously reported lead compound 1, a series of 1,2-diamino-ethane-substituted-6,7,8,9-tetrahydro-5H-pyrimido[4,5-d]azepines were synthesized and evaluated for improved physiochemical and pharmacokinetic properties while maintaining TRPV1 antagonist activity. Structure-activity relationship studies...
5.
Lebsack A, Branstetter B, Hack M, Xiao W, Peterson M, Nasser N, et al.
Bioorg Med Chem Lett
. 2008 Nov;
19(1):40-6.
PMID: 19038548
We have identified and synthesized a series of 2,7-diamino-thiazolo[5,4-d]pyrimidines as TRPV1 antagonists. An exploration of the structure-activity relationships at the 2-, 5-, and 7-positions of the thiazolo[5,4-d]pyrimidine led to the...