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Development and evaluation of a pharmacophore model for inhibitors of aldosterone synthase (CYP11B2).
Ulmschneider, Sarah; Negri, Matthias; Voets, Marieke; Hartmann, Rolf W.
Afiliación
  • Ulmschneider S; 8.2 Pharmaceutical and Medicinal Chemistry, Saarland University, PO Box 15 11 50, D-66041 Saarbrücken, Germany.
Bioorg Med Chem Lett ; 16(1): 25-30, 2006 Jan 01.
Article en En | MEDLINE | ID: mdl-16246562
Recently, we proposed inhibition of aldosterone synthase (CYP11B2) as a novel strategy for the treatment of congestive heart failure and myocardial fibrosis and synthesized a large number of inhibitors. In this work, a pharmacophore model for CYP11B2 inhibitors was developed by superimposition of active and non-active compounds. This model was confirmed by the synthesis of two pyridyl substituted acenaphthene derivatives (A,B). This new class of compounds as well as the pharmacophore could be helpful for the discovery of novel inhibitors.
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Base de datos: MEDLINE Asunto principal: Diseño de Fármacos / Química Farmacéutica / Citocromo P-450 CYP11B2 / Inhibidores Enzimáticos Tipo de estudio: Diagnostic_studies / Evaluation_studies Límite: Humans Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2006 Tipo del documento: Article País de afiliación: Alemania
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Base de datos: MEDLINE Asunto principal: Diseño de Fármacos / Química Farmacéutica / Citocromo P-450 CYP11B2 / Inhibidores Enzimáticos Tipo de estudio: Diagnostic_studies / Evaluation_studies Límite: Humans Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2006 Tipo del documento: Article País de afiliación: Alemania