Design, synthesis, and structure-activity relationship of novel CCR2 antagonists.

Kothandaraman, Shankaran; Donnely, Karla L; Butora, Gabor; Jiao, Richard; Pasternak, Alexander; Morriello, Gregori J; Goble, Stephen D; Zhou, Changyou; Mills, Sander G; Maccoss, Malcolm; Vicario, Pasquale P; Ayala, Julia M; Demartino, Julie A; Struthers, Mary; Cascieri, Margaret A; Yang, Lihu

Kothandaraman, Shankaran; Donnely, Karla L; Butora, Gabor; Jiao, Richard; Pasternak, Alexander; Morriello, Gregori J; Goble, Stephen D; Zhou, Changyou; Mills, Sander G; Maccoss, Malcolm; Vicario, Pasquale P; Ayala, Julia M; Demartino, Julie A; Struthers, Mary; Cascieri, Margaret A; Yang, Lihu.

Afiliación

Kothandaraman S; Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065, USA.

Bioorg Med Chem Lett ; 19(6): 1830-4, 2009 Mar 15.

Article en En | MEDLINE | ID: mdl-19237282

ABSTRACT

ABSTRACT

A series of novel 1-aminocyclopentyl-3-carboxyamides incorporating substituted tetrahydropyran moieties have been synthesized and subsequently evaluated for their antagonistic activity against the human CCR2 receptor. Among them analog 59 was found to posses potent antagonistic activity.

Asunto(s)

Química Farmacéutica/métodos; Receptores CCR2/antagonistas & inhibidores; Receptores CCR2/química; Administración Oral; Animales; Quimiotaxis; Perros; Diseño de Fármacos; Humanos; Concentración 50 Inhibidora; Macaca mulatta; Modelos Químicos; Estructura Molecular; Ratas; Ratas Sprague-Dawley; Relación Estructura-Actividad

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Texto completo: 1 Banco de datos: MEDLINE Asunto principal: Química Farmacéutica / Receptores CCR2 Límite: Animals / Humans Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2009 Tipo del documento: Article País de afiliación: Estados Unidos

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