R
Raffaello Masciadri
Researcher at Hoffmann-La Roche
Publications - 68
Citations - 1178
Raffaello Masciadri is an academic researcher from Hoffmann-La Roche. The author has contributed to research in topics: Alkyl & Alkoxy group. The author has an hindex of 18, co-authored 68 publications receiving 1141 citations. Previous affiliations of Raffaello Masciadri include University of Basel.
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Journal ArticleDOI
4-aminoquinoline analogs of chloroquine with shortened side chains retain activity against chloroquine-resistant Plasmodium falciparum.
Robert G. Ridley,Werner Hofheinz,Hugues Matile,Catherine Jaquet,Arnulf Dorn,Raffaello Masciadri,Synese Jolidon,Wolfgang F. Richter,A Guenzi,M A Girometta,H Urwyler,Walter Huber,S Thaithong,W Peters +13 more
TL;DR: An assessment of the activities of four selected compounds containing ethyl, propyl, and isopropyl side chains that retain activity against chloroquine-resistant isolates of Plasmodium falciparum malaria and the formation of N-dealkylated metabolites of these compounds.
Journal ArticleDOI
Characterization of (R,S)-5,7-di-tert-butyl-3-hydroxy-3-trifluoromethyl-3H-benzofuran-2-one as a positive allosteric modulator of GABAB receptors.
P. Malherbe,Raffaello Masciadri,Roger David Norcross,Frédéric Knoflach,Claudia Kratzeisen,Marie-Thérèse Zenner,Yeter Kolb,Anne Marcuz,Jörg Huwyler,T. Nakagawa,Porter Richard Hugh Phillip,Andrew Thomas,Joseph G. Wettstein,Sleight Andrew,Will Spooren,Eric Prinssen +15 more
TL;DR: The aim of this study was to characterize derivatives of (R,S)‐5,7‐di‐tert‐butyl‐ 3‐hydroxy‐3‐trifluoromethyl‐3H‐benzofuran‐2‐one (rac‐BHFF) as enhancers of GABAB receptors.
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Hematin Polymerization Assay as a High-Throughput Screen for Identification of New Antimalarial Pharmacophores
Yae Kurosawa,Arnulf Dorn,Michiko Kitsuji-Shirane,Michiko Kitsuji-Shirane,Hisao Shimada,Tomoko Satoh,Tomoko Satoh,Hugues Matile,Werner Hofheinz,Raffaello Masciadri,Manfred Kansy,Robert G. Ridley,Robert G. Ridley +12 more
TL;DR: A high-throughput in vitro microassay of hematin polymerization based on the detection of 14C-labeled heme incorporated into polymeric hemozoin (malaria pigment) that could form the basis of a new antimalarial medicinal chemistry program.
Journal ArticleDOI
New vistas in quinoline synthesis
Sarkis Atechian,Nadine Nock,Roger David Norcross,Hassen Ratni,Andrew Thomas,Julien Verron,Raffaello Masciadri +6 more
TL;DR: The gold-catalyzed Friedlander reaction was applied to the condensation of 2-aminoarylketones with β-keto-esters, β-diketones and β-amides.
Journal ArticleDOI
Antimalarial activity of the bisquinoline trans-N1,N2-bis (7-chloroquinolin-4-yl)cyclohexane-1,2-diamine: comparison of two stereoisomers and detailed evaluation of the S,S enantiomer, Ro 47-7737.
Robert G. Ridley,Hugues Matile,Catherine Jaquet,Arnulf Dorn,Werner Hofheinz,Werner Leupin,Raffaello Masciadri,F P Theil,Wolfgang F. Richter,M A Girometta,A Guenzi,H Urwyler,E Gocke,J M Potthast,M Csato,A Thomas,W Peters +16 more
TL;DR: The S,S enantiomer of the bisquinoline trans-N1,N2-bis(7-chloroquinolin-4-yl)cyclohexane-1,2-diamine, Ro 47-7737, is significantly more potent against chloroquine-resistant Plasmodium falciparum than the R,R enantiomers and the racemate, and can be explained in part by its long terminal half-life.