Zobrazeno 1 - 10
of 17
pro vyhledávání: '"Serge Belanger"'
Autor:
Guo-Hua Chu, William M. Barker, Rolf T. Windh, Patrick J. Little, Michael J. Derelanko, Bertrand Le Bourdonnec, Michael Koblish, Diane L. DeHaven-Hudkins, Minghua Gu, Thomas M. Graczyk, Daniel D. Wiant, Lara K. Leister, Bernice L. Brogdon, Robert N. DeHaven, Christopher W. Ajello, Steven A. Smith, Serge Belanger, David D. Christ, Paul A. Tuthill, Steve Kutz, Joel A. Cassel, Marina S. Feschenko, Roland E. Dolle
Publikováno v:
Journal of Medicinal Chemistry. 51:5893-5896
Selective delta opioid receptor agonists are promising potential therapeutic agents for the treatment of various types of pain conditions. A spirocyclic derivative was identified as a promising hit through screening. Subsequent lead optimization iden
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::619e8cbfdd85472b2463e048206eebc5
https://doi.org/10.1021/jm8008986
https://doi.org/10.1021/jm8008986
Autor:
Roland E. Dolle, Diane L. DeHaven-Hudkins, Daniel D. Wiant, Joel A. Cassel, William M. Barker, Patrick J. Little, Bertrand Le Bourdonnec, Robert N. DeHaven, Serge Belanger, Nathalie Conway-James, Timothy J. O’Neill
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:2006-2012
A series of N-substituted trans-3,4-dimethyl-4-(3-hydroxyphenyl)piperidines, mu opioid receptor antagonists, analogs of alvimopan, were prepared using solid phase methodology. This study led to the identification of a highly selective mu opioid recep
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b26c41c2d45b977ff06a701c18afedae
https://doi.org/10.1016/j.bmcl.2008.01.106
https://doi.org/10.1016/j.bmcl.2008.01.106
Autor:
Michael Koblish, Minghua Gu, Thomas M. Graczyk, Patrick J. Little, Nathalie Conway-James, Robert N. DeHaven, Serge Belanger, Diane L. DeHaven-Hudkins, Guo-Hua Chu, Joel A. Cassel, Roland E. Dolle
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:1951-1955
A novel series of malonamide derivatives was synthesized. These amides were shown to be potent and selective kappa opioid receptor agonists.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::32ad212de03125134561624676bd1165
https://doi.org/10.1016/j.bmcl.2007.01.053
https://doi.org/10.1016/j.bmcl.2007.01.053
Autor:
Serge Belanger, Roland E. Dolle, Christopher W. Ajello, Bertrand Le Bourdonnec, Roberta G. Susnow, Pamela R. Seida, Robert N. DeHaven, Diane L. DeHaven-Hudkins, Gabriel J. Stabley, Joel A. Cassel
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 15:2647-2652
Some kappa opioid receptor agonists of the arylacetamide class, for example, ICI 199441 (1), were found to strongly inhibit the activity of cytochrome P450 2D6 (CYP2D6) (1: CYP2D6 IC50=26 nM). Certain analogs bearing a substituted sulfonylamino group
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4f421d8b56811acaf0d1070cfa53aedd
https://doi.org/10.1016/j.bmcl.2005.03.020
https://doi.org/10.1016/j.bmcl.2005.03.020
Autor:
Serge Belanger, William M. Barker, Patrick J. Little, Pamela R. Seida, Roland E. Dolle, Paul A. Tuthill, Michael Koblish, Joel A. Cassel, Susan L. Gottshall, Robert N. DeHaven, Diane L. DeHaven-Hudkins
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 14:5693-5697
A new class of kappa-opioid receptor agonists is described. The design of these agents was based upon energy minimization and structural overlay studies of the generic azepin-2-one structure 3 with the crystal structure of arylacetamide kappa agonist
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8a510b8869767016eef7e278505207c4
https://doi.org/10.1016/j.bmcl.2004.08.041
https://doi.org/10.1016/j.bmcl.2004.08.041
Autor:
Mathieu Machaut, Joel A. Cassel, Gabriel J. Stabley, Robert N. DeHaven, Roland E. Dolle, Thomas M. Graczyk, Blanca Martinez-Teipel, Serge Belanger
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 14:3545-3548
( S )-4-(Carboxamido)phenylalanine (Cpa) is examined as a bioisosteric replacement for the terminal tyrosine (Tyr) residue in a variety of known peptide ligands for the μ , δ , and κ opioid receptors. The Cpa-containing peptides, assayed against c
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::63288140e896f649e1bebb0082a4e2f1
https://doi.org/10.1016/j.bmcl.2004.04.039
https://doi.org/10.1016/j.bmcl.2004.04.039
Publikováno v:
European Journal of Neuroscience. 13:1125-1135
Chronic pain caused by nerve injury and inflammation is more common in the elderly. However, mechanisms underlying this phenomenon are unclear. Higher sensitivity of sensory neurons to free radicals has been suggested as one possibility. The producti
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::d623a7ad8be564ca1652e2afd6cb12fb
https://doi.org/10.1046/j.1460-9568.2001.01475.x
https://doi.org/10.1046/j.1460-9568.2001.01475.x
Autor:
Thomas M. Graczyk, Patrick J. Little, Diane L. DeHaven-Hudkins, William M. Barker, Michael Koblish, Rolf T. Windh, Minghua Gu, Marina S. Feschenko, Joel A. Cassel, Guo-Hua Chu, Daniel D. Wiant, Steve Kutz, Lara Kathryn Leister, Robert N. DeHaven, Serge Belanger, Bertrand Le Bourdonnec, Roland E. Dolle, Bernice L. Brogdon, Steven A. Smith, Tuthill Paul Anson, Michael J. Derelanko, Q. Jean Zhou, Christopher W. Ajello
Publikováno v:
Journal of medicinal chemistry. 52(18)
Selective, nonpeptidic delta opioid receptor agonists have been the subject of great interest as potential novel analgesic agents. The discoveries of BW373U86 (1) and SNC80 (2) contributed to the rapid expansion of research in this field. However, po
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::bfc53d00daff04ac1abedc34cfddc85c
https://pubmed.ncbi.nlm.nih.gov/19694468
https://pubmed.ncbi.nlm.nih.gov/19694468
Autor:
Allan J. Goodman, Serge Belanger, Robert N. DeHaven, Pamela R. Seida, Thomas M. Graczyk, Bertrand Le Bourdonnec, Roland E. Dolle
Publikováno v:
Journal of medicinal chemistry. 49(25)
To better understand structural requirements for a mu ligand of the trans-3,4-dimethyl-4-(3-hydroxyphenyl)piperidine class to interact with the mu opioid receptor, we have described in the previous article (Le Bourdonnec, B. et al. J. Med. Chem. 2006
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e679225be6390e4cec8a40dc299743c5
https://pubmed.ncbi.nlm.nih.gov/17149859
https://pubmed.ncbi.nlm.nih.gov/17149859
Autor:
Thomas M. Graczyk, Mathieu Michaut, Robert N. DeHaven, Serge Belanger, Blanca Martinez-Teipel, Roland E. Dolle
Publikováno v:
Bioorganicmedicinal chemistry letters. 17(9)
A series of opioid peptide ligands containing modified N-terminal tyrosine (Tyr) residues was prepared and evaluated against cloned human mu, delta, and kappa opioid receptors. This work extends the recent discovery that (S)-4-carboxamidophenylalanin
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::bfba88d5cdea83c4d6b89a9f12558ffd
https://pubmed.ncbi.nlm.nih.gov/17350835
https://pubmed.ncbi.nlm.nih.gov/17350835