Výsledky vyhledávání - "Joseph R. Fotsing"

Akademický článek

Toxicological evaluation of the flavour ingredient N-(1-((4-amino-2,2-dioxido-1H-benzo[c][1,2,6]thiadiazin-5-yl)oxy)-2-methylpropan-2-yl)-2,6-dimethylisonicotinamide (S2218)

Autor: Donald S. Karanewsky, Guy Servant, Hanghui Liu, Bert Chi, Lily Ida, Michael Saganich, Sara Werner, Joseph R. Fotsing, Andrew Patron, Catherine Tachdjian, Amy Arthur

Publikováno v: Toxicology Reports, Vol 4, Iss , Pp 507-520 (2017)

A toxicological evaluation of N-(1-((4-amino-2,2-dioxido-1H-benzo[c][1,2,6]thiadiazin-5-yl)oxy)-2-methylpropan-2-yl)-2,6-dimethylisonicotinamide (S2218; CAS 1622458-34-7), a flavour with modifying properties, was completed for the purpose of assessin

Externí odkaz: https://doaj.org/article/e104bf811a6b41778b1fd0b467f96e72

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Discovery and Development of S6821 and S7958 as Potent TAS2R8 Antagonists

Autor: Lan Zhang, Hanghui Liu, Brett Weylan Ching, Guy Servant, Tanya Ditschun, Andrew Patron, Thomas Brady, Mark C. Williams, Melissa Arellano, Vincent Darmohusodo, Michael Saganich, Qing Chen, Timothy Davis, Catherine Tachdjian, Donald S. Karanewsky, Joseph R. Fotsing

Publikováno v: Journal of medicinal chemistry. 63(9)

In humans, bitter taste is mediated by 25 TAS2Rs. Many compounds, including certain active pharmaceutical ingredients, excipients, and nutraceuticals, impart their bitter taste (or in part) through TAS2R8 activation. However, effective TAS2R8 blocker

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d3bf37e3c7509316160de3e35812932e
https://pubmed.ncbi.nlm.nih.gov/32330040

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Toxicological evaluation of the flavour ingredient N -(1-((4-amino-2,2-dioxido-1 H -benzo[ c ][1,2,6]thiadiazin-5-yl)oxy)-2-methylpropan-2-yl)-2,6-dimethylisonicotinamide (S2218)

Autor: Bert Chi, Andrew Patron, Michael Saganich, Sara Werner, Catherine Tachdjian, Guy Servant, Amy J. Arthur, Joseph R. Fotsing, Lily Ida, Hanghui Liu, Donald S. Karanewsky

Publikováno v: Toxicology Reports, Vol 4, Iss, Pp 507-520 (2017)
Toxicology Reports

Graphical abstract The results of the ADME, genotoxicity, rodent toxicology and developmental toxicology studies conducted on a new flavour compound S2218 are reported. S2218 is a positive allosteric modifier (PAM) of the human sweet taste receptor a

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::bcdef84c8da13f7445a16395430628f3
https://doi.org/10.1016/j.toxrep.2017.09.004

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Synthesis of Selective Agonists for the α7 Nicotinic Acetylcholine Receptor with In Situ Click-Chemistry on Acetylcholine-Binding Protein Templates

Autor: Kwok-Yiu Ho, K. Barry Sharpless, Neil P. Grimster, Mikael Dufouil, Todd T. Talley, Kimberly Gomez, Palmer Taylor, Valery V. Fokin, John G. Yamauchi, Akos Nemecz, Joseph R. Fotsing

Publikováno v: Molecular Pharmacology. 82:687-699

The acetylcholine-binding proteins (AChBPs), which serve as structural surrogates for the extracellular domain of nicotinic acetylcholine receptors (nAChRs), were used as reaction templates for in situ click-chemistry reactions to generate a congener

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d046e32717174debae934038c192e2e7
https://doi.org/10.1124/mol.112.080291

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Generation of Candidate Ligands for Nicotinic Acetylcholine Receptors via in situ Click Chemistry with a Soluble Acetylcholine Binding Protein Template

Autor: K. Barry Sharpless, Kwok-Yiu Ho, Neil P. Grimster, John G. Yamauchi, Akos Nemecz, Timo Weide, Choel Kim, Bernhard Stump, Palmer Taylor, Joseph R. Fotsing, Valery V. Fokin, Todd T. Talley

Publikováno v: Journal of the American Chemical Society. 134:6732-6740

Nicotinic acetylcholine receptors (nAChRs), which are responsible for mediating key physiological functions, are ubiquitous in the central and peripheral nervous systems. As members of the Cys loop ligand-gated ion channel family, neuronal nAChRs are

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::62476b7929cbf760f8ee0dc8f4901291
https://doi.org/10.1021/ja3001858

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Inhibitors of VIM-2 by screening pharmacologically active and click-chemistry compound libraries

Autor: Michael Spaargaren, K. Barry Sharpless, Moreno Galleni, S. Adrian Saldanha, Patricia Lassaux, Timothy P. Spicer, Peter Hodder, Prem S. Subramaniam, Joseph R. Fotsing, Timo Weide, Carine Bebrone, Dmitriy Minond, Valery V. Fokin

Publikováno v: Bioorganic & Medicinal Chemistry. 17:5027-5037

VIM-2 is an Ambler class B metallo-beta-lactamase (MBL) capable of hydrolyzing a broad-spectrum of beta-lactam antibiotics. Although the discovery and development of MBL inhibitors continue to be an area of active research, an array of potent, small

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e20c29e7320018d33d62c0290c7abe2f
https://doi.org/10.1016/j.bmc.2009.05.070

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Photolysis of open-chain 1,2-diazidoalkenes: generation of 2-azido-2H-azirines, formyl cyanide, and formyl isocyanide

Autor: Günther Maier, Manfred Hagedorn, Joseph R. Fotsing, Klaus Banert, Hans Peter Reisenauer

Publikováno v: Tetrahedron. 64:5645-5648

Solutions of several open-chain 1,2-diazidoethenes were photolyzed to yield 2-azido-2 H -azirines, which were identified by NMR spectroscopy at low temperature. On prolonged irradiation or warm-up of the NMR solutions, these heterocycles lost a secon

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::155d3428126aa8ba8934f4a8b880e3a2
https://doi.org/10.1016/j.tet.2008.04.037

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New Way to Methylene-2H-azirines and Their Use as Powerful Intermediates for the Stereo- and Regioselective Synthesis of Compounds with Vinylamine Substructure

Autor: Klaus Banert, Joseph R. Fotsing

Publikováno v: European Journal of Organic Chemistry. 2006:3617-3625

New and relatively stable methylene-2H-azirines 1 have been prepared by photolysis of allenyl azides or from 2-halo-2H-azirines by elimination of HX (X = halogen). The reaction of these methylene-2H-azirines with nucleophiles led to the highly stereo

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::7c5d3f97abe8205fe40d5cf9255a528e
https://doi.org/10.1002/ejoc.200600302

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Reactions of Unsaturated Azides; Part 17:An Efficient Strategy for the Synthesis of Small-Ring Heterocycles via Isomerization of 2-Halo-2H-azirines

Autor: Joseph R. Fotsing, Klaus Banert

Publikováno v: Synthesis. :261-272

New acceptor-substituted allenyl halides were synthesized. The addition of hydrazoic acid (HN 3 ) to these allenyl halides led to the formation of new 1-azido-2-haloethene derivatives. The photolysis of the latter compounds afforded the corresponding

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0d69afa7bca297d5f936936468ef3a88
https://doi.org/10.1055/s-2005-918513

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First successful synthesis, isolation and characterization of open-chain 1,2-diazidoethenes

Autor: Klaus Banert, Manfred Hagedorn, Joseph R. Fotsing

Publikováno v: Tetrahedron. 61:8904-8909

Open-chain 1,2-diazidoethenes have been obtained from the recently reported acceptor-substituted propargyl azides by one-pot reactions with tetramethylguanidinium azide (TMGA) and in some cases via a two-step procedure starting with in situ productio

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::5426ac32edf5a964a9548b2f0afdcf5c
https://doi.org/10.1016/j.tet.2005.07.025

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