The SAR studies of novel CB2 selective agonists, benzimidazolone derivatives.

Omura, Hirofumi; Kawai, Makoto; Shima, Akiko; Iwata, Yasuhiro; Ito, Fumitaka; Masuda, Tsutomu; Ohta, Atsuko; Makita, Naoya; Omoto, Kiyoyuki; Sugimoto, Hiromi; Kikuchi, Akira; Iwata, Hiroshi; Ando, Kazuo

Omura, Hirofumi; Kawai, Makoto; Shima, Akiko; Iwata, Yasuhiro; Ito, Fumitaka; Masuda, Tsutomu; Ohta, Atsuko; Makita, Naoya; Omoto, Kiyoyuki; Sugimoto, Hiromi; Kikuchi, Akira; Iwata, Hiroshi; Ando, Kazuo.

Afiliação

Omura H; Discovery Chemistry Research, Pfizer Global Research & Development, Nagoya Laboratories, Pfizer Japan Inc., 5-2 Taketoyo, Aichi 470-2393, Japan. omurah@gmail.com

Bioorg Med Chem Lett ; 18(11): 3310-4, 2008 Jun 01.

Article em En | MEDLINE | ID: mdl-18440813

ABSTRACT

ABSTRACT

Benzimidazolone derivatives were discovered as novel CB2 selective agonists. Structure Activity Relationship (SAR) studies around them were examined to improve metabolic stability. Compound 39 exhibited excellent metabolic stability in human liver microsomes (HLM) and significant attenuation of the chronic colonic allodynia in the TNBS-treated rats by po administration.

Assuntos

Benzimidazóis/síntese química; Benzimidazóis/farmacologia; Receptor CB2 de Canabinoide/agonistas; Animais; Benzimidazóis/química; Técnicas de Química Combinatória; Desenho de Fármacos; Humanos; Estrutura Molecular; Ratos; Receptor CB1 de Canabinoide/agonistas; Relação Estrutura-Atividade

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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Benzimidazóis / Receptor CB2 de Canabinoide Limite: Animals / Humans Idioma: En Ano de publicação: 2008 Tipo de documento: Article

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