Výsledky vyhledávání - "Christopher W. Ajello"

Novel sulfamoyl benzamides as selective CB2 agonists with improved in vitro metabolic stability

Autor: Patrick J. Little, Joel A. Cassel, Allan J. Goodman, Lara K. Leister, Ian Sellitto, Markku A. Savolainen, Christopher J. LaBuda, Robert N. DeHaven, Karin Worm, Steven A. Smith, Christopher W. Ajello, Bertrand Le Bourdonnec, Roland E. Dolle, Christopher T. Saeui, Michael Koblish, Bernice L. Brogdon, Guo-Hua Chu

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 20:387-391

A lead optimization campaign in our previously reported sulfamoyl benzamide class of CB2 agonists was conducted to improve the in vitro metabolic stability profile in this series while retaining high potency and selectivity for the CB2 receptor. From

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d579866e08bfd69294c876bac2b8e941
https://doi.org/10.1016/j.bmcl.2009.10.062

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Design and Synthesis of Imidazopyrimidine Derivatives as Potent iNOS Dimerization Inhibitors

Autor: Tuthill Paul Anson, Minghua Gu, Joel A. Cassel, Ian Sellitto, Lara Kathryn Leister, Heather O’ Hare, Guo-Hua Chu, Christopher W. Ajello, Roland E. Dolle, Robert N. DeHaven, Bertrand Le Bourdonnec

Publikováno v: The Open Medicinal Chemistry Journal

A series of imidazopyrimidine derivatives with the general formula I was synthesized and identified as potent inhibitors of iNOS dimer formation, a prerequisite for proper functioning of the enzyme. Stille and Negishi coupling reactions were used as

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9539aaf781f867a97c4dc52f43008ea4
https://doi.org/10.2174/1874104500903010008

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Nascent structure–activity relationship study of a diastereomeric series of kappa opioid receptor antagonists derived from CJ-15,208

Autor: Patrick J. Carroll, Pamela R. Seida, Mathieu Michaut, Alison L. Muller, Roland E. Dolle, Robert N. DeHaven, Christopher W. Ajello, Blanca Martinez-Teipel

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 19:3647-3650

Cyclic tetrapeptide c[Phe-pro-Phe-trp] 2, a diastereomer of CJ-15,208 (1), was identified as a potent dual kappa/mu opioid receptor antagonist devoid of delta opioid receptor affinity against cloned human receptors: K(i) (2)=3.8nM (kappa), 30nM (mu);

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::69ceebfdc49e6c33d085494bccaf4d0d
https://doi.org/10.1016/j.bmcl.2009.04.105

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CB2 selective sulfamoyl benzamides: Optimization of the amide functionality

Autor: Bertrand Le Bourdonnec, Patrick J. Little, Christopher W. Ajello, Bernice L. Brogdon, Markku A. Savolainen, Steven A. Smith, Michael Koblish, Allan J. Goodman, Christopher J. LaBuda, Robert N. DeHaven, Heather O’Hare, Roland E. Dolle, Joel A. Cassel, Karin Worm, Gabriel J. Stabley

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 19:309-313

Previous research within our laboratories identified sulfamoyl benzamides as novel cannabinoid receptor ligands. Optimization of the amide linkage led to the reverse amide 40. The compound exhibited robust antiallodynic activity in a rodent pain mode

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d4aec622684e4b3c4e447395c83cae23
https://doi.org/10.1016/j.bmcl.2008.11.091

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Potent, Orally Bioavailable Delta Opioid Receptor Agonists for the Treatment of Pain: Discovery of N,N-Diethyl-4-(5-hydroxyspiro[chromene-2,4′-piperidine]-4-yl)benzamide (ADL5859)

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

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Arylacetamide κ opioid receptor agonists with reduced cytochrome P450 2D6 inhibitory activity

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

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Spirocyclic delta opioid receptor agonists for the treatment of pain: discovery of N,N-diethyl-3-hydroxy-4-(spiro[chromene-2,4'-piperidine]-4-yl) benzamide (ADL5747)

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

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Akademický článek

Spirocyclic Delta Opioid Receptor Agonists for the Treatment of Pain: Discovery of N,N-Diethyl-3-hydroxy-4-(spiro[chromene-2,4′-piperidine]-4-yl) Benzamide (ADL5747).

Publikováno v: Journal of Medicinal Chemistry; Sep2009, Vol. 52 Issue 18, p5685-5702, 18p

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