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Design, synthesis and evaluation of phenethylaminoheterocycles as K(v)1.5 inhibitors.
Johnson, James A; Xu, Ningning; Jeon, Yoon; Finlay, Heather J; Kover, Alexander; Conder, Mary L; Sun, Huabin; Li, Danshi; Levesque, Paul; Hsueh, Mei-Mann; Harper, Timothy W; Wexler, Ruth R; Lloyd, John.
Afiliación
  • Johnson JA; Department of Discovery Chemistry, Bristol-Myers Squibb Research and Development, PO Box 5400, Princeton, NJ 08534-5400, USA. Electronic address: james.a.johnson@bms.com.
  • Xu N; Department of Discovery Chemistry, Bristol-Myers Squibb Research and Development, PO Box 5400, Princeton, NJ 08534-5400, USA.
  • Jeon Y; Department of Discovery Chemistry, Bristol-Myers Squibb Research and Development, PO Box 5400, Princeton, NJ 08534-5400, USA.
  • Finlay HJ; Department of Discovery Chemistry, Bristol-Myers Squibb Research and Development, PO Box 5400, Princeton, NJ 08534-5400, USA.
  • Kover A; Department of Discovery Chemistry, Bristol-Myers Squibb Research and Development, PO Box 5400, Princeton, NJ 08534-5400, USA.
  • Conder ML; Department of Discovery Biology, Bristol-Myers Squibb Research and Development, PO Box 5400, Princeton, NJ 08534-5400, USA.
  • Sun H; Department of Discovery Biology, Bristol-Myers Squibb Research and Development, PO Box 5400, Princeton, NJ 08534-5400, USA.
  • Li D; Department of Discovery Biology, Bristol-Myers Squibb Research and Development, PO Box 5400, Princeton, NJ 08534-5400, USA.
  • Levesque P; Department of Discovery Biology, Bristol-Myers Squibb Research and Development, PO Box 5400, Princeton, NJ 08534-5400, USA.
  • Hsueh MM; Department of Preclinical Candidate Optimization, Bristol-Myers Squibb Research and Development, PO Box 5400, Princeton, NJ 08534-5400, USA.
  • Harper TW; Department of Preclinical Candidate Optimization, Bristol-Myers Squibb Research and Development, PO Box 5400, Princeton, NJ 08534-5400, USA.
  • Wexler RR; Department of Discovery Chemistry, Bristol-Myers Squibb Research and Development, PO Box 5400, Princeton, NJ 08534-5400, USA.
  • Lloyd J; Department of Discovery Chemistry, Bristol-Myers Squibb Research and Development, PO Box 5400, Princeton, NJ 08534-5400, USA.
Bioorg Med Chem Lett ; 24(14): 3018-22, 2014 Jul 15.
Article en En | MEDLINE | ID: mdl-24881565
Phenethylaminoheterocycles have been prepared and assayed for inhibition of the Kv1.5 potassium ion channel as a potential approach to the treatment of atrial fibrillation. A diverse set of heterocycles were identified as potent Kv1.5 inhibitors and were advanced to pharmacodynamic evaluation based on selectivity and pharmacokinetic profile. Heterocycle optimization and template modification lead to the identification of compound 24 which demonstrated increased atrial effective refractory period in the rabbit pharmacodynamic model with mild effects on blood pressure and heart rate.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Carbamatos / Diseño de Fármacos / Bloqueadores de los Canales de Potasio / Canal de Potasio Kv1.5 / Indazoles Límite: Animals / Humans Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2014 Tipo del documento: Article Pais de publicación: Reino Unido
Texto completo
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Carbamatos / Diseño de Fármacos / Bloqueadores de los Canales de Potasio / Canal de Potasio Kv1.5 / Indazoles Límite: Animals / Humans Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2014 Tipo del documento: Article Pais de publicación: Reino Unido