Discovery of 2-(4-((1H-1,2,4-triazol-1-yl)methyl)-5-(4-bromophenyl)-1-(2-chlorophenyl)-1H-pyrazol-3-yl)-5-tert-butyl-1,3,4-thiadiazole (GCC2680) as a potent, selective and orally efficacious cannabinoid-1 receptor antagonist.

Lee, Jinhwa; Seo, Hee Jeong; Lee, Suk Ho; Kim, Jeongmin; Jung, Myung Eun; Lee, Sung-Han; Song, Kwang-Seop; Lee, Junwon; Kang, Suk Youn; Kim, Min Ju; Kim, Mi-Soon; Son, Eun-Jung; Lee, Minwoo; Han, Ho-Kyun

Lee, Jinhwa; Seo, Hee Jeong; Lee, Suk Ho; Kim, Jeongmin; Jung, Myung Eun; Lee, Sung-Han; Song, Kwang-Seop; Lee, Junwon; Kang, Suk Youn; Kim, Min Ju; Kim, Mi-Soon; Son, Eun-Jung; Lee, Minwoo; Han, Ho-Kyun.

Afiliação

Lee J; Research Center, Green Cross Corporation, 303 Bojeong-dong, Giheung-gu, Yongin 446-770, Republic of Korea. jinhwa_2_lee@hotmail.com

Bioorg Med Chem ; 18(17): 6377-88, 2010 Sep 01.

Article em En | MEDLINE | ID: mdl-20673729

Assuntos

Receptor CB1 de Canabinoide/antagonistas & inibidores; Tiadiazóis/farmacologia; Animais; Células CHO; Cricetinae; Cricetulus; Humanos; Masculino; Camundongos; Camundongos Endogâmicos C57BL; Obesidade/tratamento farmacológico; Ratos; Ratos Sprague-Dawley; Receptor CB1 de Canabinoide/química; Relação Estrutura-Atividade; Tiadiazóis/síntese química; Tiadiazóis/química; Tiadiazóis/farmacocinética

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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Tiadiazóis / Receptor CB1 de Canabinoide Limite: Animals / Humans / Male Idioma: En Ano de publicação: 2010 Tipo de documento: Article

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