Structure-activity relationships of novel non-competitive mGluR1 antagonists: a potential treatment for chronic pain.

Owen, Dafydd R; Dodd, Peter G; Gayton, Simon; Greener, Ben S; Harbottle, Gareth W; Mantell, Simon J; Maw, Graham N; Osborne, Simon A; Rees, Huw; Ringer, Tracy J; Rodriguez-Lens, Margarita; Smith, Graham F

Owen, Dafydd R; Dodd, Peter G; Gayton, Simon; Greener, Ben S; Harbottle, Gareth W; Mantell, Simon J; Maw, Graham N; Osborne, Simon A; Rees, Huw; Ringer, Tracy J; Rodriguez-Lens, Margarita; Smith, Graham F.

Afiliación

Owen DR; Pfizer Global Research and Development, Ramsgate Road, Sandwich, CT13 9NJ, UK. dafydd.owen@pfizer.com

Bioorg Med Chem Lett ; 17(2): 486-90, 2007 Jan 15.

Article en En | MEDLINE | ID: mdl-17064898

RESUMEN

A series of novel mGluR1 antagonists have been prepared. Incorporation of fragments derived from weak lead matter into a library led to enhanced potency in a new chemical series. A chemistry driven second library iteration, covering a greatly enhanced area of chemical space, maintained good potency and introduced metabolic stability.

Asunto(s)

Dolor/tratamiento farmacológico; Receptores de Glutamato Metabotrópico/antagonistas & inhibidores; Animales; Unión Competitiva/efectos de los fármacos; Células CHO; Fenómenos Químicos; Química Física; Enfermedad Crónica; Cricetinae; Cricetulus; Relación Dosis-Respuesta a Droga; Ácido Glutámico/farmacología; Pirazinas/síntesis química; Pirazinas/farmacología; Ratas; Relación Estructura-Actividad

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Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Dolor / Receptores de Glutamato Metabotrópico Límite: Animals Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2007 Tipo del documento: Article Pais de publicación: Reino Unido

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