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Jones, Philip S; Boucharens, Sylviane; McElroy, Stuart P; Morrison, Angus; Honarnejad, Saman; van Boeckel, Stan; van den Hurk, Helma; Basting, Daniel; Hüser, Jörg; Jaroch, Stefan; Ottow, Eckhard; Benningshof, Jorg; Folmer, Rutger H A; Leemhuis, Frank; Kramer-Verhulst, Patricia M; Nies, Vera J M; Orrling, Kristina M; Rijnders, Ton; Pfander, Claudia; Engkvist, Ola; Pairaudeau, Garry; Simpson, Peter B; Ortholand, Jean-Yves; Roche, Didier; Dömling, Alexander; Kühnert, Sven M; Roevens, Peter W M; van Vlijmen, Herman; van Wanrooij, Eva J A; Verbruggen, Christophe; Nussbaumer, Peter; Ovaa, Huib; van der Stelt, Mario; Simonsen, Klaus Baek; Tagmose, Lena; Waldmann, Herbert; Duffy, James; Finsinger, Dirk; Jurzak, Mirek; Burgess-Brown, Nicola A; Lee, Wen H; Rutjes, Floris P J T; Haag, Hubert; Kallus, Christopher; Mors, Hartmut; Dorval, Thierry; Lesur, Brigitte; Ramon Olayo, Fernando; Hamza, Daniel; Jones, Geraint.

Nat Rev Drug Discov ; 21(4): 245-246, 2022 04.

Artículo en Inglés | MEDLINE | ID: mdl-34907316

Asunto(s)

Ensayos Analíticos de Alto Rendimiento , Bibliotecas de Moléculas Pequeñas , Descubrimiento de Drogas , Humanos

alpha-Cycloalkyl-substituted omega-keto-dicarboxylic acids as lipid regulating agents.

Bell, Roel P L; Verdijk, Dennis; Relou, Mike; Smith, Dennis; Regeling, Henk; Ebbers, Eelco J; Leemhuis, Frank M C; Oniciu, Daniela C; Cramer, Clay T; Goetz, Brian; Pape, Michael E; Krause, Brian R; Bisgaier, Charles L; Dasseux, Jean-Louis.

Bioorg Med Chem ; 13(1): 223-36, 2005 Jan 03.

Artículo en Inglés | MEDLINE | ID: mdl-15582467

RESUMEN

A series of cycloalkyl-substituted oxo-alkanedicarboxylic acids have been prepared by the TosMIC methodology departing from haloalkyl-substituted cycloalkylcarboxylic esters. cyclopropyl derivatives showed IC(50) activity in the 0.3-1.0 microM range on the de novo incorporation of radiolabeled acetate into lipids in primary cultures of rat hepatocytes, and they showed lipid-regulating properties when tested in vivo in female obese Zucker fatty rats.

Asunto(s)

Ácidos Dicarboxílicos/farmacología , Lípidos/sangre , Lipoproteínas/sangre , Animales , Células Cultivadas , Ácidos Dicarboxílicos/química , Hepatocitos/efectos de los fármacos , Hepatocitos/metabolismo , Espectroscopía de Resonancia Magnética , Masculino , Espectrometría de Masas , Ratas , Ratas Sprague-Dawley

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