Výsledky vyhledávání - "Edwin J Schweiger"

Liver X Receptor (LXR) partial agonists: Biaryl pyrazoles and imidazoles displaying a preference for LXRβ

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 25:372-377

A series of biaryl pyrazole and imidazole Liver X Receptor (LXR) partial agonists has been synthesized displaying LXRβ selectivity. The LXRβ selective partial agonist 18 was identified with potent induction of ATP binding transporters ABCA1 and ABC

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7244efc41c2284fe9a58be668b38fd90
https://doi.org/10.1016/j.bmcl.2014.11.029

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5-[(2-Methyl-1,3-thiazol-4-yl)ethynyl]-2,3′-bipyridine: a highly potent, orally active metabotropic glutamate subtype 5 (mGlu5) receptor antagonist with anxiolytic activity

Autor: Benito Munoz, Jeffrey Roger Roppe, Jeffery J. Anderson, Edwin J. Schweiger, Janice Chung, Merryl Cramer, Grace Reyes-Manalo, Lida Tehrani, Xiaohui Jiang, Nicholas D. P. Cosford, Bowei Wang, Theodore M. Kamenecka, Jesse Brodkin, Dehua Huang

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 14:3993-3996

Structure-activity relationship studies leading to the discovery of a new, orally active mGlu5 receptor antagonist are described. The title compound, 5-[(2-methyl-1,3-thiazol-4-yl)ethynyl]-2,3'-bipyridine, is highly potent in vitro, has good in vivo

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e0ed6369ce4ac35bdb8054a29f2c002b
https://doi.org/10.1016/j.bmcl.2004.05.037

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Design and Synthesis of a Competent Pyrrolinone−Peptide Hybrid Ligand for the Class II Major Histocompatibility Complex Protein HLA-DR1

Autor: Amos B. Smith, Donald C. Cox, Robert M. Campbell, Gary L. Olson, Edwin J. Schweiger, Ralph Hirschmann, Mark C. Guzman, J. Barbosa, Paul A. Sprengeler, Andrew B. Benowitz, Zoltan A. Nagy, David R. Bolin

Publikováno v: Journal of the American Chemical Society. 121:9286-9298

The design and synthesis of two pyrrolinone−peptide hybrid ligands (3 and 20) for the rheumatoid arthritis-associated class II MHC HLA-DR1 protein are described. The hybrids incorporate bispyrrolinones 4 and 21 as tetrapeptide mimics for amino acid

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::80ce30b2f72fcb6060c2e697efb6fdc2
https://doi.org/10.1021/ja991251e

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Synthesis of a C, D Ring Analog of 17-α-Hydroxyprogesterone

Autor: Paul B. Weisz, Edwin J Schweiger, Madeleine M. Joullié

Publikováno v: Tetrahedron Letters. 38:6127-6130

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::2e443d32bd8c588c2d6020fcac407a5a
https://doi.org/10.1016/s0040-4039(97)01389-0

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Chemical and pharmacological characterization of galanthamine, an acetylcholinesterase inhibitor, and its derivatives. A potential application in Alzheimer's disease?

Autor: Edwin J. Schweiger, B. M. Davis, Gianluigi Forloni, E. S. Bachman, Madeleine M. Joullié, Joseph T. Coyle, So-Yeop Han, Joanne E. Sweeney

Publikováno v: European Journal of Medicinal Chemistry. 27:673-687

We conducted structural and pharmacological studies of galanthamine, a cortical acetylcholinesterase (AChE) inhibitor, and 19 structural analogs. Systematic derivatization of galanthamine at the cyclohexene ring, tertiary amino, hydroxyl and methoxyl

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::5bee74411144089019b71606b453647c
https://doi.org/10.1016/0223-5234(92)90087-h

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Cyclohexenyl- and dehydropiperidinyl-alkynyl pyridines as potent metabotropic glutamate subtype 5 (mGlu5) receptor antagonists

Autor: Grace Reyes-Manalo, Edwin J. Schweiger, Mitchell D. Green, Janice Chung, Christopher D. King, Johnny Yasuo Nagasawa, Nicholas D. P. Cosford, Peter C. Chua, Jeffrey Anderson, Merryl Cramer, Lida Tehrani, Benito Munoz, Leo Bleicher

Publikováno v: Bioorganicmedicinal chemistry letters. 15(20)

Structure-activity relationship studies leading to the discovery of novel mGlu5 receptor antagonists are described. These compounds show high in vitro potency, have good in vivo receptor occupancy, and a reasonable intravenous pharmacokinetic profile

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3bf2af7dcd707b2687a6250d8287bd3d
https://pubmed.ncbi.nlm.nih.gov/16115767

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3-[(2-Methyl-1,3-thiazol-4-yl)ethynyl]-pyridine: a potent and highly selective metabotropic glutamate subtype 5 receptor antagonist with anxiolytic activity

Autor: Jesse Brodkin, Jeffrey Roger Roppe, Linda J. Bristow, Jeffrey Anderson, Edwin J. Schweiger, Lida Tehrani, Mark S. Washburn, Ian A. McDonald, Sara Rao, Xiaohui Jiang, Nicholas D. P. Cosford, Mark A. Varney, Nicholas D. Smith

Publikováno v: Journal of medicinal chemistry. 46(2)

2-Methyl-6-(phenylethynyl)pyridine (3), a potent noncompetitive mGlu5 receptor antagonist widely used to characterize the pharmacology of mGlu5 receptors, suffers from a number of shortcomings as a therapeutic agent, including off-target activity and

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7d27cfade402b20125b94652651c157c
https://pubmed.ncbi.nlm.nih.gov/12519057

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Synthesis and biological activity of galanthamine derivatives as acetylcholinesterase (AChE) inhibitors

Autor: Bonnie M. Davis, S. C. Mayer, So-Yeop Han, Edwin J. Schweiger, Madeleine M. Joulleé

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 1:579-580

The syntheses of several ester and carbamate derivatives of galanthamine are described. These compounds are potential therapeutic agents in the treatment of Alzheimer's disease (AD). The inhibition of cortical acetylcholinesterase (AChE) by these dru

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::444a38589c6e23d29f4653e23438a516
https://doi.org/10.1016/s0960-894x(01)81154-9

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