Výsledky vyhledávání - "Jean-Paul Daris"

Synthesis and KCNQ2 opener activity of N-(1-benzo[1,3]dioxol-5-yl-ethyl, N-[1-(2,3-dihydro-benzofuran-5-yl)-ethyl, and N-[1-(2,3-dihydro-1H-indol-5-yl)-ethyl acrylamides

Autor: Jean-Paul Daris, John E. Starrett, Pierre Dextraze, Rick L. Pieschl, Huan He, David G. Harden, David Weaver, Jie Chen, Yong-Jin Wu, Ronald J. Knox, Valentin K. Gribkoff, Li-Qiang Sun, Qi Gao, Mark W. Thompson, Dedong Wu, Christopher G. Boissard, Steven I. Dworetzky, William Fitzpatrick, JoAnne E Natale

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 14:4533-4537

Bioisosteric replacement studies led to the identification of N -(1-benzo[1,3]dioxol-5-yl-ethyl)-3-(2-chloro-phenyl)-acrylamide (( S )- 3 ) as a highly potent KCNQ2 opener, and 3-(2,6-difluoro-phenyl)- N -[1-(2,3-dihydro-benzofuran-5-yl)-ethyl]-acryl

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ca337a8d17cff2971f2f629786972798
https://doi.org/10.1016/j.bmcl.2004.06.035

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Novel mimics of sialyl Lewis X

Autor: Wright John J, Brigitte Turmel, Serge Plamondon, Kenneth M. Tramposch, Paul L. Stanley, Alain Martel, Pierre Dextraze, Carol Bachand, Julie Alford, Carl Ouellet, Marcel Menard, Anne Marinier, Gordon Todderud, Jacques Banville, Jean-Paul Daris, Debbie Lee, Philippe Lapointe, Xina Nair

Publikováno v: Bioorganic & Medicinal Chemistry. 9:1395-1427

A series of potent inhibitors of P-selectin as potential anti-inflammatory agents is reported. These compounds are derivatives of galactocerebrosides bearing a malonate side chain in positions 2 and 3 of the galactose moiety. Based on the binding mod

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::f3f94f1486084c27529de687fb62c136
https://doi.org/10.1016/s0968-0896(01)00015-3

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BMS-200475, a novel carbocyclic 2′-deoxyguanosine analog with potent and selective anti-hepatitis B virus activity in vitro

Autor: G. A. Jacobs, S. Innaimo, William A. Slusarchyk, O. Kocy, J.E. Sundeen, Robert Zahler, Alain Martel, M. G. Young, Sam T. Chao, Jean-Paul Daris, Gregory S. Bisacchi, Richard J. Colonno, C. Bachard, Philippe Lapointe, Z. Merchant

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 7:127-132

BMS-200475, a novel carbocyclic analog of 2′-deoxyguanosine, is a potent inhibitor of hepatitis B virus in vitro (ED50 = 3 nM) with relatively low cytotoxicity (CC50 = 21–120 μM). A practical 10-step asymmetric synthesis was developed affording

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::4f254f1ed35e99aef5acd2c244ca770e
https://doi.org/10.1016/s0960-894x(96)00594-x

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New azole antagonists with high affinity for the P2Y(1) receptor

Autor: Patrick Y.S. Lam, Jean-Paul Daris, Carl Thibeault, Ruth R. Wexler, Ji Hua, Robert P. Rehfuss, Qimin Wu, Alexandre L'Heureux, Alain Martel, Rejean Ruel, Laura Price

Publikováno v: Bioorganicmedicinal chemistry letters. 23(12)

Five-membered-ring heterocyclic urea mimics have been found to be potent and selective antagonists of the P2Y1 receptor. SAR of the various heterocyclic replacements is presented, as well as side-chain SAR of the more potent thiadiazole ring system w

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::94869f87bcf45a4fbf5948460f5776ea
https://pubmed.ncbi.nlm.nih.gov/23668989

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Nuclear analogs of β-lactam antibiotics. XVI. Aldol condensations of N-protected 4-tritylthio-2-azetidinones

Autor: Alain Martel, Bernard Belleau, Jean Collerette, Jean-Paul Daris, Philippe Lapointe, Marcel Menard, Banville Jacques

Publikováno v: Canadian Journal of Chemistry. 61:613-618

The reaction of acetaldehyde with enolates of N-protected 4-tritylthio-2-azetidinones 4b and 4c was studied. While the lithium enolate of N-methoxymethylazetidinone 4b gave only transS* 3-(1′-hydroxyethyl)azetidinone 8 the corresponding tetrabutyla

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::6d90d686782a547390a205cf4c12ec7b
https://doi.org/10.1139/v83-111

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Phenyl group as a probe in the 1H nuclear magnetic resonance study of the conformations of quaternary heteroaromatic carbapenem antibiotics. Identification of the site of quaternization in -SCH2- substituted nitrogen-containing heteroaromatic derivatives

Autor: Jean-Paul Daris, Marcel Menard, Vanga S. Rao

Publikováno v: Canadian Journal of Chemistry. 66:1546-1551

The phenyl group is shown as a useful probe in sensing the environment in the 1H nuclear magnetic resonance conformational study of a variety of quaternary heteroaromatic carbapenem derivatives. The influence of the -SCH2- substituent in determining

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::1efe823249733abc41557dbbc609b936
https://doi.org/10.1139/v88-251

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Ring C substituted 14-hydroxymorphinans and isomorphinans as narcotic antagonists

Autor: Yvon G. Perron, Marcel Menard, Pierre Rivest, Jean-Paul Daris, Bernard Belleau

Publikováno v: Canadian Journal of Chemistry. 54:429-439

The synthesis of morphinans incorporating a hydroxyl group at position 14 as well as an appropriate alkyl substitution in ring C is described. It is shown that the spatial area around ring C plays an important role at the analgesic receptor level. A

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::7c8e0e7da37d8a774d8b9abcf504f049
https://doi.org/10.1139/v76-059

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5-Allyl-9-oxobenzomorphans. Part 4. Synthesis of 3-hydroxy-8-oxyisomorphinans, 5-allyl-9α-hydroxy-6,7-benzomorphans, and related tetrahydrofuranobenzomorphans

Autor: Yvon Lambert, Ivo Monkovic, Jean-Paul Daris

Publikováno v: Canadian Journal of Chemistry. 55:2523-2529

A series of 3-hydroxy-8-oxyisomorphinans (11, 16) has been synthesized from the corresponding 5-allyl-9β-hydroxy-6,7-benzomorphans (7, 12) via a hydroboration, oxidation, mesylation, and cyclization sequence of reactions. Selective reduction of and

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::8388504a3d039197d58d02749be433e7
https://doi.org/10.1139/v77-347

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The Photochemical Isomerization of N-Bromo-α,β-unsaturated Lactams; An Intermolecular Allylic Bromination Process Involving a Probable Bromine Radical Chain

Autor: Ercole Cavalieri, Jean-Paul Daris, Denis Gravel, Jacques Hebert, Jacques Bilodeau

Publikováno v: Canadian Journal of Chemistry. 52:645-652

The photochemical behavior of the N-bromo-α,β-unsaturated lactams 1b and 2b has been investigated with particular regard to their potential intramolecular reactions. In both cases the main product corresponds to an isomerization of bromine to the 5

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::b56e329e2e74cd5434edea6b9417ef93
https://doi.org/10.1139/v74-099

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