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.

Afiliação

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 em 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.

Assuntos

Química Farmacêutica/métodos; Receptores CCR2/antagonistas & inibidores; Receptores CCR2/química; Administração Oral; Animais; Quimiotaxia; Cães; Desenho de Fármacos; Humanos; Concentração Inibidora 50; Macaca mulatta; Modelos Químicos; Estrutura Molecular; Ratos; Ratos Sprague-Dawley; Relação Estrutura-Atividade

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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Química Farmacêutica / Receptores CCR2 Limite: Animals / Humans Idioma: En Ano de publicação: 2009 Tipo de documento: Article

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