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James J Folmer

Explore the profile of James J Folmer including associated specialties, affiliations and a list of published articles. Areas
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Recent Articles
1.
Brown D, Bernstein P, Griffin A, Wesolowski S, Labrecque D, Tremblay M, et al.
J Med Chem . 2014 Jan; 57(3):733-58. PMID: 24410637
A new series of potent and selective histamine-3 receptor (H3R) antagonists was identified on the basis of an azaspiro[2.5]octane carboxamide scaffold. Many scaffold modifications were largely tolerated, resulting in nanomolar-potent...
2.
Yu J, Folmer J, Hoesch V, Doherty J, Campbell J, Burdette D
Drug Metab Dispos . 2010 Nov; 39(2):302-11. PMID: 21045198
Studies on the biotransformation of isoxazole rings have shown that molecules containing a C3-substituted isoxazole or a 1,2-benzisoxazole can undergo a two-electron reductive ring cleavage to form an imine. In...
3.
Brugel T, Smith R, Balestra M, Becker C, Daniels T, Hoerter T, et al.
Bioorg Med Chem Lett . 2010 Aug; 20(19):5847-52. PMID: 20727752
Initial high throughput screening efforts identified highly potent and selective kappa opioid receptor antagonist 3 (κ IC(50)=77 nM; μ:κ and δ:κ IC(50) ratios>400) which lacked CNS exposure in vivo. Modification...
4.
Scott C, Sobotka-Briner C, Wilkins D, Jacobs R, Folmer J, Frazee W, et al.
J Pharmacol Exp Ther . 2002 Dec; 304(1):433-40. PMID: 12490620
Caspase-3 is an intracellular cysteine protease, activated as part of the apoptotic response to cell injury. Its interest as a therapeutic target has led many to pursue the development of...