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Synthesis and immunostimulatory activity of 8-substituted amino 9-benzyladenines as potent Toll-like receptor 7 agonists.
Bioorg Med Chem Lett
September 2006
Moores Cancer Center, University of California, San Diego, La Jolla, 92093-0820, USA.
Several 9-benzyl adenine derivatives bearing various substituted amines at the 8-position have been prepared and evaluated for interferon induction in peripheral blood mononuclear cells (PBMC) from healthy human donors. The 8-bromoadenine derivative 5 was used as a versatile intermediate for all substitutions. The most active 8-substituted amino compound was found to be the 8-morpholinoethylamino derivative 19 which had an EC(50) in the submicromolar range.
View Article and Find Full Text PDFSynthesis and biological evaluation of 2,8-disubstituted 9-benzyladenines: discovery of 8-mercaptoadenines as potent interferon-inducers.
Bioorg Med Chem
July 2003
Laboratory of Medicinal Chemistry, Gifu Pharmaceutical University, 5-6-1 Mitahora-higashi, Gifu 502-8585, Japan.
Recently, we have identified 9-benzyl-8-hydroxyadenines bearing an appropriate substituent (a butoxy, propylthio or butylamino group) at the 2-position as potent interferon (IFN)-inducers. Herein we report the design, synthesis, and IFN-inducing activity of 8-substituted 9-benzyladenines possessing such an appropriate substituent at the 2-position. Introduction of the appropriate substituent into the 2-position of the adenine nucleus gave rise to expression of the activity even in 9-benzyladenines bearing no hydroxyl group at the 8-position.
View Article and Find Full Text PDFAnti-TNF-alpha properties of new 9-benzyladenine derivatives with selective phosphodiesterase-4- inhibiting properties.
Biochem Biophys Res Commun
October 2001
Laboratoire de Pharmacologie et Physico-Chimie des Interactions Cellulaires et Moléculaires (UMR 7034 du CNRS), Université Louis Pasteur de Strasbourg, UFR de Sciences Pharmaceutiques, 74 route du Rhin, 67401 Illkirch Cedex, France.
In inflammatory cells, intracellular cAMP concentration is regulated by cyclic nucleotide phosphodiesterases 4. Therefore, PDE4 inhibition appears as a rational goal for treating acute or chronic inflammatory diseases. Selective PDE4 inhibitors have been developed, but due to unwanted side effects, search for new selective PDE4-inhibitors had to be pursued.
View Article and Find Full Text PDF9-Benzyladenines: potent and selective cAMP phosphodiesterase inhibitors.
J Med Chem
June 1997
Laboratoire de Pharmacochimie Moléculaire, UPR 421 du CNRS, Strasbourg, France.
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