Výsledky vyhledávání - "Heather Twin"

A hydrogen borrowing annulation strategy for the stereocontrolled synthesis of saturated aza-heterocycles

Autor: Heather Twin, Timothy J. Donohoe, Roly J. Armstrong, Anna E. R. Chamberlain, Kieran J. Paterson

Publikováno v: Chemical Communications. 56:3563-3566

An iridium catalyzed method for the synthesis of saturated aza-heterocycles from amines and diols is reported. A wide range of substituted heterocycles can be obtained using this approach including products bearing substituents at the C2, C3 and C4 p

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::80ce2abe39ecbe0f141fb112fdcd0b7e
https://doi.org/10.1039/d0cc00903b

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Strategies for the modulation of phase II metabolism in a series of PKCε inhibitors

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 24:3398-3402

Extensive phase II metabolism of an advanced PKCε inhibitor resulted in sub-optimal pharmacokinetics in rat marked by elevated clearance. Synthesis of the O-glucuronide metabolite as a standard was followed by three distinct strategies to specifical

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::76338524c1b4881c748508cd81b19f7b
https://doi.org/10.1016/j.bmcl.2014.05.082

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Substituted 2,5-diazabicyclo[4.1.0]heptanes and their application as general piperazine surrogates: synthesis and biological activity of a Ciprofloxacin analogue

Autor: Rivka R. R. Taylor, Rebecca J. Mallot, Heather Twin, Wendy Wen, Robert A. Batey, Alan J. Lough, Scott D. Gray-Owen

Publikováno v: Tetrahedron. 66:3370-3377

Piperazines and modified piperazines, such as homopiperazines and 2-methylpiperazines, are found in a wide range of pharmaceutical substances and biologically active molecules. In this study 2,5-diazabicyclo[4.1.0]heptanes, in which a cyclopropane ri

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::ae34e777cbbad184e36918c172b85a5e
https://doi.org/10.1016/j.tet.2010.02.046

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A biogenetically inspired heterodimerization approach to the synthesis of the core structure of the alkaloid fissoldhimine

Autor: Wendy Wen, Heather Twin, David A. Powell, Robert A. Batey, Alan J. Lough

Publikováno v: Tetrahedron Letters. 48:1841-1844

A biogenetically inspired heterodimerization reaction of N-substituted 2-pyrroline equivalents leads to the tricyclic core of the alkaloid fissoldhimine. Thus, pyrrolidin-2-ol derivatives, in which the nitrogen atom is substituted either with urea or

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::e20441182f5f4a49906db43f0291cbc3
https://doi.org/10.1016/j.tetlet.2007.01.019

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Design and optimization of selective protein kinase C θ (PKCθ) inhibitors for the treatment of autoimmune diseases

Autor: Damien Fraysse, Peter Chiu, Philip N. Collier, Heather Twin, Luca Settimo, Francoise Pierard, Dean Boyall, Shazia Keily, Claire M. Bolton, Christopher John Davis, Guy Brenchley, Adam P. Curnock, Jaclyn Henderson, Adam Tanner, Juan-Miguel Jimenez, Andrew Miller, Stephen Clinton Young

Publikováno v: Journal of medicinal chemistry. 56(5)

Protein kinase C θ (PKCθ) has a central role in T cell activation and survival; however, the dependency of T cell responses to the inhibition of this enzyme appears to be dictated by the nature of the antigen and by the inflammatory environment. St

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e18d0371ff520503045d7d7722ddbc9b
https://pubmed.ncbi.nlm.nih.gov/23442161

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Discovery and structure-activity relationship of 3-aminopyrid-2-ones as potent and selective interleukin-2 inducible T-cell kinase (Itk) inhibitors

Autor: Heather Twin, Adam Tanner, David Kay, Adam P. Curnock, Juan-Miguel Jimenez, Sharn Ramaya, Ronald Knegtel, Guy Brenchley, Shazia Keily, Andrew Miller, Jean-Damien Charrier, Steven Durrant, Philip N. Collier, Kieron Brown

Publikováno v: Journal of medicinal chemistry. 54(7)

Interleukin-2 inducible T-cell kinase (Itk) plays a role in T-cell functions, and its inhibition potentially represents an attractive intervention point to treat autoimmune and allergic diseases. Herein we describe the discovery of a series of potent

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f6e13363387677c2554b66abc10b740a
https://pubmed.ncbi.nlm.nih.gov/21391610

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ChemInform Abstract: Asymmetric Synthesis of 2-Substituted Piperidines Using a Multi-Component Coupling Reaction: Rapid Assembly of (S)-Coniine from (S)-1-(1-Phenylethyl)-2-methyleneaziridine

Autor: Heather Twin, Jerome F. Hayes, Michael Shipman

Publikováno v: ChemInform. 33

(S)-Coniine is made using a reaction which assembles the piperidine ring by the sequential formation of four new chemical bonds and installs the C-2 stereogenic centre with high levels of diastereocontrol (90% de).

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::187daab517218a44592ee7587f04c9ff
https://doi.org/10.1002/chin.200202231

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