Výsledky vyhledávání - "Thomas Stephen Coulter"

The discovery of an orally efficacious positive allosteric modulator of the calcium sensing receptor containing a dibenzylamine core

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 20:5544-5547

The discovery of a series of novel and orally efficacious type II calcimimetics, developed from the lead compound 1, is described herein. Compound 22 suppressed plasma PTH levels relative to vehicle when dosed orally in a rat pharmacodynamic model.

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e863f669015b2935d346cb0793aca12e
https://doi.org/10.1016/j.bmcl.2010.07.060

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HCV NS5B polymerase inhibitors 2: Synthesis and in vitro activity of (1,1-dioxo-2H-[1,2,4]benzothiadiazin-3-yl) azolo[1,5-a]pyridine and azolo[1,5-a]pyrimidine derivatives

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 19:4480-4483

(1,1-Dioxo-2H-[1,2,4]benzothiadiazin-3-yl) azolo[1,5-a]pyridine and azolo[1,5-a]pyrimidine derivatives have been investigated as potential anti-HCV drugs. Their synthesis, HCV NS5B polymerase inhibition, and replicon activity are discussed.

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::000ef0a9262fe818849b255d0368b7bd
https://doi.org/10.1016/j.bmcl.2009.05.022

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Inhibitors of HIV-1 attachment. Part 8: the effect of C7-heteroaryl substitution on the potency, and in vitro and in vivo profiles of indole-based inhibitors

Publikováno v: Bioorganicmedicinal chemistry letters. 23(1)

As part of the SAR profiling of the indole-oxoacetic piperazinyl benzamide class of HIV-1 attachment inhibitors, substitution at the C7 position of the lead 4-fluoroindole 2 with various 5- and 6-membered heteroaryl moieties was explored. Highly pote

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::077777990fa95df55f4fc3845cd0e4b4
https://pubmed.ncbi.nlm.nih.gov/23200249

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The synthesis and evaluation of indolylureas as PKCα inhibitors

Autor: Richard John Mears, Songtao Zhou, Thomas Stephen Coulter, Christian A.G.N. Montalbetti, Oliver Barker, Jane Far-Jine Djung, Adam Golebiowski, Gregory F. Davis, Elizabeth Dolan, Kenneth D. Greis, Andrew N. Carr

Publikováno v: Bioorganicmedicinal chemistry. 19(8)

PKCα and PKA have crucial but opposing roles in the regulation of calcium handling within myocytes. Identification of compounds that inhibit PKCα, but not PKA, are potential therapeutic targets for the treatment of heart disease. The synthesis of i

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b4ffb63c05e15e55ac7feeff6fe0ef3e
https://pubmed.ncbi.nlm.nih.gov/21435888

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Syntheses and antiproliferative evaluation of oxyphenisatin derivatives

Autor: Thomas Stephen Coulter, Serge G. Reignier, Christian A.G.N. Montalbetti, Charlotta Grånäs, Steven Butcher, Christian Krog-Jensen, Muhammed Kamal Uddin, Jakob Felding

Publikováno v: Bioorganicmedicinal chemistry letters. 17(10)

Syntheses and structure-antiproliferative relationship for oxyphenisatin analogues are described. The cell proliferation data showed that the presence of substituents (especially F, Cl, Me, CF(3), and OMe) in the 6- and 7-position of oxyphenisatin ma

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::441ea4b0cf7819e31986794c189daae3
https://pubmed.ncbi.nlm.nih.gov/17368900

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