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Page 1
Discovery and Characterization of ACT-451840: an Antimalarial Drug with a Novel Mechanism of Action.
Boss C, Aissaoui H, Amaral N, Bauer A, Bazire S, Binkert C, Brun R, Bürki C, Ciana CL, Corminboeuf O, Delahaye S, Dollinger C, Fischli C, Fischli W, Flock A, Frantz MC, Girault M, Grisostomi C, Friedli A, Heidmann B, Hinder C, Jacob G, Le Bihan A, Malrieu S, Mamzed S, Merot A, Meyer S, Peixoto S, Petit N, Siegrist R, Trollux J, Weller T, Wittlin S. Boss C, et al. Among authors: siegrist r. ChemMedChem. 2016 Sep 20;11(18):1995-2014. doi: 10.1002/cmdc.201600298. Epub 2016 Jul 29. ChemMedChem. 2016. PMID: 27471138
Identification of a new chemical class of antimalarials.
Brunner R, Aissaoui H, Boss C, Bozdech Z, Brun R, Corminboeuf O, Delahaye S, Fischli C, Heidmann B, Kaiser M, Kamber J, Meyer S, Papastogiannidis P, Siegrist R, Voss T, Welford R, Wittlin S, Binkert C. Brunner R, et al. Among authors: siegrist r. J Infect Dis. 2012 Sep 1;206(5):735-43. doi: 10.1093/infdis/jis418. Epub 2012 Jun 25. J Infect Dis. 2012. PMID: 22732921
Novel in vivo active anti-malarials based on a hydroxy-ethyl-amine scaffold.
Ciana CL, Siegrist R, Aissaoui H, Marx L, Racine S, Meyer S, Binkert C, de Kanter R, Fischli C, Wittlin S, Boss C. Ciana CL, et al. Among authors: siegrist r. Bioorg Med Chem Lett. 2013 Feb 1;23(3):658-62. doi: 10.1016/j.bmcl.2012.11.118. Epub 2012 Dec 11. Bioorg Med Chem Lett. 2013. PMID: 23260352
UV-triggered affinity capture identifies interactions between the Plasmodium falciparum multidrug resistance protein 1 (PfMDR1) and antimalarial agents in live parasitized cells.
Brunner R, Ng CL, Aissaoui H, Akabas MH, Boss C, Brun R, Callaghan PS, Corminboeuf O, Fidock DA, Frame IJ, Heidmann B, Le Bihan A, Jenö P, Mattheis C, Moes S, Müller IB, Paguio M, Roepe PD, Siegrist R, Voss T, Welford RW, Wittlin S, Binkert C. Brunner R, et al. Among authors: siegrist r. J Biol Chem. 2013 Aug 2;288(31):22576-83. doi: 10.1074/jbc.M113.453159. Epub 2013 Jun 10. J Biol Chem. 2013. PMID: 23754276 Free PMC article.
Discovery of substituted lactams as novel dual orexin receptor antagonists. Synthesis, preliminary structure-activity relationship studies and efforts towards improved metabolic stability and pharmacokinetic properties. Part 1.
Sifferlen T, Boller A, Chardonneau A, Cottreel E, Hoecker J, Aissaoui H, Williams JT, Brotschi C, Heidmann B, Siegrist R, Gatfield J, Treiber A, Brisbare-Roch C, Jenck F, Boss C. Sifferlen T, et al. Among authors: siegrist r. Bioorg Med Chem Lett. 2014 Feb 15;24(4):1201-8. doi: 10.1016/j.bmcl.2013.12.092. Epub 2013 Dec 30. Bioorg Med Chem Lett. 2014. PMID: 24447850
Structure-activity relationship, biological, and pharmacological characterization of the proline sulfonamide ACT-462206: a potent, brain-penetrant dual orexin 1/orexin 2 receptor antagonist.
Boss C, Roch-Brisbare C, Steiner MA, Treiber A, Dietrich H, Jenck F, von Raumer M, Sifferlen T, Brotschi C, Heidmann B, Williams JT, Aissaoui H, Siegrist R, Gatfield J. Boss C, et al. Among authors: siegrist r. ChemMedChem. 2014 Nov;9(11):2486-96. doi: 10.1002/cmdc.201402258. Epub 2014 Aug 21. ChemMedChem. 2014. PMID: 25147058
Structure-Activity Relationship, Drug Metabolism and Pharmacokinetics Properties Optimization, and in Vivo Studies of New Brain Penetrant Triple T-Type Calcium Channel Blockers.
Siegrist R, Pozzi D, Jacob G, Torrisi C, Colas K, Braibant B, Mawet J, Pfeifer T, de Kanter R, Roch C, Kessler M, Moon R, Corminboeuf O, Bezençon O. Siegrist R, et al. J Med Chem. 2016 Dec 8;59(23):10661-10675. doi: 10.1021/acs.jmedchem.6b01356. Epub 2016 Nov 23. J Med Chem. 2016. PMID: 27933950
The Screening Compound Collection: A Key Asset for Drug Discovery.
Boss C, Hazemann J, Kimmerlin T, von Korff M, Lüthi U, Peter O, Sander T, Siegrist R. Boss C, et al. Among authors: siegrist r. Chimia (Aarau). 2017 Oct 25;71(10):667-677. doi: 10.2533/chimia.2017.667. Chimia (Aarau). 2017. PMID: 29070412 Free article.
Milestones to the Discovery of T-type Calcium Channel Blockers for the Treatment of Generalized Epilepsies.
Bezençon O, Siegrist R, Heidmann B, Pozzi D, Stamm S, Remeň L, Richard S, Simons L, Gaston R, Downing D, Grisostomi C, Roch C, Kessler M, Gatfield J, Moon R, Pfeifer T, Mosbacher J, Reymond I, Ertel EA, de Kanter R, Capeleto B, Fournier E, Rey M, Moccia L, Toeroek-Schafroth M, Roscher R, Schindelholz B. Bezençon O, et al. Among authors: siegrist r. Chimia (Aarau). 2017 Oct 25;71(10):722-729. doi: 10.2533/chimia.2017.722. Chimia (Aarau). 2017. PMID: 29070417 Free article.
69 results