Zobrazeno 1 - 10
of 14
pro vyhledávání: '"John Paul Kilburn"'
Autor:
Suresh Poda, Robb Brodbeck, Veena Menon, Manuel Cajina, Elena Dale, Annemette V. Thougaard, Martin Juhl, Londye Calice, Hopper Allen T, Thomas Möller, Roland G. W. Staal, Michel Grenon, Stevin H. Zorn, Kenneth A. Jones, Gamini Chandrasena, Tanzilya Khayrullina, Jorrit J. Hornberg, Lassina Badolo, John Paul Kilburn, Dekun Song, Adarsh Gandhi, Megan Nattini, Hong Zhang, Christian Thomsen, Gennady N. Smagin
Publikováno v:
Journal of Medicinal Chemistry. 64:4891-4902
There remains an insufficient number of P2X7 receptor antagonists with adequate rodent potency, CNS permeability, and pharmacokinetic properties from which to evaluate CNS disease hypotheses preclinically. Herein, we describe the molecular pharmacolo
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b10e3f87ae056269e65ef5baa722afdf
https://doi.org/10.1021/acs.jmedchem.0c02249
https://doi.org/10.1021/acs.jmedchem.0c02249
Publikováno v:
Bioorganic & Medicinal Chemistry. 23:4453-4461
The application of BN/CC isosterism is explored as a method of expanding the scope of core scaffolds in biologically active compounds. The viability of potential drug candidates incorporating BN-heteroaromatic moieties was investigated through the sy
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fa1d626e7021712477aea37438f0a530
https://doi.org/10.1016/j.bmc.2015.06.019
https://doi.org/10.1016/j.bmc.2015.06.019
Autor:
Andreas Ritzen, Christoffer Bundgaard, Farah Mohamed M, Claus Tornby Christoffersen, John Paul Kilburn, Morten Langgård, Jacob Nielsen, Jan Kehler, Sebastian Leth Petersen
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:3738-3742
Novel triazoloquinazolines have been found as phosphodiesterase 10A (PDE10A) inhibitors. Structure–activity studies improved the initial micromolar potency which was found in the lead compound by a 100-fold identifying 5-(1H-benzoimidazol-2-ylmethy
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e9436fcf472e4b5503c730939b373fc8
https://doi.org/10.1016/j.bmcl.2011.04.067
https://doi.org/10.1016/j.bmcl.2011.04.067
Autor:
John Paul Kilburn, Jan Kehler
Publikováno v:
Expert Opinion on Therapeutic Patents. 19:1715-1725
PDE10A inhibition has generated much excitement as a potential novel mechanism for the treatment of the positive symptoms of schizophrenia. PDE10A is only '10 years old' as a drug discovery target since it was first discovered in 1999, and thus PDE10
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b6bfcae175b44b83fc3e005c9d627c2e
https://doi.org/10.1517/13543770903431050
https://doi.org/10.1517/13543770903431050
Publikováno v:
Tetrahedron. 61:5565-5575
New robust protocols for the solid phase synthesis of 5-alkylthio-, 5-alkyl/aryl-, and 5-acylamino-2-alkylamino-[1,3,4]-thiadiazoles are described based on a common resin bound thiosemicarbazide. A protocol for the solid phase synthesis of 2-alkyl/ar
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::43c1df8732a65fdedcff229872d148cc
https://doi.org/10.1016/j.tet.2005.03.084
https://doi.org/10.1016/j.tet.2005.03.084
Publikováno v:
Organic Letters. 6:19-22
[reaction: see text] Highly functionalized l-serine-derived organolithium reagents have been generated and reacted with a variety of electrophiles, delivering novel enantiomerically pure adducts. These adducts were then converted into homochiral amin
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::58840f82c226bd46b93e0e7a5166317a
https://doi.org/10.1021/ol0360039
https://doi.org/10.1021/ol0360039
Publikováno v:
Tetrahedron Letters. 44:7825-7828
Two novel and facile syntheses strategies for the synthesis of substituted 1,3,4-thiadiazoles on solid support are described based on a resin-bound thiosemicarbazide: (a) treatment with aldehydes to form immobilised thiosemicarbazones, and oxidative
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::6ce267438fcefa9947b4993857466de4
https://doi.org/10.1016/j.tetlet.2003.08.077
https://doi.org/10.1016/j.tetlet.2003.08.077
Autor:
Yu Ge, Jesper Lau, Roy Teruyuki Uyeda, Henrik Sune Andersen, Daniel D. Holsworth, John Paul Kilburn, Luke M. Judge, Karla Frydenvang, Thomas Kruse Hansen
Publikováno v:
Tetrahedron. 58:7339-7344
A convenient large-scale chiral synthesis of protected 2-substituted-4-oxo-piperidine derivatives is described. Hetero Diels–Alder reaction between trifluoroacetic acid–boron trifluoride activated (1-phenyl-ethylimino)acetic acid ethyl ester and
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::3902572f3cbf71572c7e74b1c1823e49
https://doi.org/10.1016/s0040-4020(02)00682-8
https://doi.org/10.1016/s0040-4020(02)00682-8
Publikováno v:
Tetrahedron. 58:1739-1743
A new facile solid-phase synthesis of N,N′,N″-substituted guanidines from an immobilised amine component is described. The resin-bound amine was reacted with di-(2-pyridyl)thionocarbonate to generate the isothiocyanate which was treated with aryl
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::1c0c3be9e4d29b91cc05f08ecf54fd8b
https://doi.org/10.1016/s0040-4020(02)00033-9
https://doi.org/10.1016/s0040-4020(02)00033-9
Autor:
Claus Tornby Christoffersen, John Paul Kilburn, Benny Bang-Andersen, Christoffer Bundgaard, Søren Rahn Christensen, Alf Thibblin, Stine Timmermann, Mads Kreilgaard, Jan Kehler, Bjoern Steiniger-Brach, Gunnar Antoni, Jacob Nielsen, Mark Lubberink, Lise T. Brennum, Sergio Estrada, Anders Wall
Publikováno v:
Journal of nuclear medicine : official publication, Society of Nuclear Medicine. 55(9)
Phosphodiesterase 10A (PDE10A) plays a key role in the regulation of brain striatal signaling, and several pharmaceutical companies currently investigate PDE10A inhibitors in clinical trials for various central nervous system diseases. A PDE10A PET l
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9416b831cfef1e586dc68ee60d6137cd
https://pubmed.ncbi.nlm.nih.gov/24994928
https://pubmed.ncbi.nlm.nih.gov/24994928