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Benzimidazole-carboxamides as potent and bioavailable stearoyl-CoA desaturase (SCD1) inhibitors from ligand-based virtual screening and chemical optimization.
Matter, Hans; Zoller, Gerhard; Herling, Andreas W; Sanchez-Arias, Juan-Antonio; Philippo, Christophe; Namane, Claudie; Kohlmann, Markus; Pfenninger, Anja; Voss, Marc D.
Afiliação
  • Matter H; Sanofi-Aventis Deutschland GmbH, Research and Development, D-65926 Frankfurt am Main, Germany. Hans.Matter@sanofi.com
Bioorg Med Chem Lett ; 23(6): 1817-22, 2013 Mar 15.
Article em En | MEDLINE | ID: mdl-23395660
ABSTRACT
The discovery of potent benzimidazole stearoyl-CoA desaturase (SCD1) inhibitors by ligand-based virtual screening is described. ROCS 3D-searching gave a favorable chemical motif that was subsequently optimized to arrive at a chemical series of potent and promising SCD1 inhibitors. In particular, compound SAR224 was selected for further pharmacological profiling based on favorable in vitro data. After oral administration to male ZDF rats, this compound significantly decreased the serum fatty acid desaturation index, thus providing conclusive evidence for SCD1 inhibition in vivo by SAR224.
Assuntos

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Estearoil-CoA Dessaturase / Tiofenos / Benzimidazóis / Inibidores Enzimáticos / Amidas Tipo de estudo: Diagnostic_studies / Screening_studies Limite: Animals / Humans / Male Idioma: En Revista: Bioorg Med Chem Lett Assunto da revista: BIOQUIMICA / QUIMICA Ano de publicação: 2013 Tipo de documento: Article País de afiliação: Alemanha

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Estearoil-CoA Dessaturase / Tiofenos / Benzimidazóis / Inibidores Enzimáticos / Amidas Tipo de estudo: Diagnostic_studies / Screening_studies Limite: Animals / Humans / Male Idioma: En Revista: Bioorg Med Chem Lett Assunto da revista: BIOQUIMICA / QUIMICA Ano de publicação: 2013 Tipo de documento: Article País de afiliação: Alemanha