A novel series of 4-methyl substituted pyrazole derivatives as potent glucagon receptor antagonists: Design, synthesis and evaluation of biological activities.

Shu, Shuangjie; Dai, Antao; Wang, Jiang; Wang, Bin; Feng, Yang; Li, Jia; Cai, Xiaoqing; Yang, Dehua; Ma, Dakota; Wang, Ming-Wei; Liu, Hong

Shu, Shuangjie; Dai, Antao; Wang, Jiang; Wang, Bin; Feng, Yang; Li, Jia; Cai, Xiaoqing; Yang, Dehua; Ma, Dakota; Wang, Ming-Wei; Liu, Hong.

Afiliação

Shu S; State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 555 Zu Chong Zhi Road, Shanghai 201203, China; The CAS Key Laboratory of Receptor Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences (CAS), 555 Zu Chong Zhi Road, Shangh
Dai A; The National Center for Drug Screening, 189 Guo Shou Jing Road, Shanghai 201203, China.
Wang J; State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 555 Zu Chong Zhi Road, Shanghai 201203, China; The CAS Key Laboratory of Receptor Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences (CAS), 555 Zu Chong Zhi Road, Shangh
Wang B; State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 555 Zu Chong Zhi Road, Shanghai 201203, China; The CAS Key Laboratory of Receptor Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences (CAS), 555 Zu Chong Zhi Road, Shangh
Feng Y; The National Center for Drug Screening, 189 Guo Shou Jing Road, Shanghai 201203, China.
Li J; State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 555 Zu Chong Zhi Road, Shanghai 201203, China; The CAS Key Laboratory of Receptor Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences (CAS), 555 Zu Chong Zhi Road, Shangh
Cai X; The National Center for Drug Screening, 189 Guo Shou Jing Road, Shanghai 201203, China.
Yang D; The CAS Key Laboratory of Receptor Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences (CAS), 555 Zu Chong Zhi Road, Shanghai 201203, China; The National Center for Drug Screening, 189 Guo Shou Jing Road, Shanghai 201203, China.
Ma D; The National Center for Drug Screening, 189 Guo Shou Jing Road, Shanghai 201203, China.
Wang MW; The CAS Key Laboratory of Receptor Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences (CAS), 555 Zu Chong Zhi Road, Shanghai 201203, China; The National Center for Drug Screening, 189 Guo Shou Jing Road, Shanghai 201203, China; School of Pharmacy, Fudan University, 826 Zhang
Liu H; State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 555 Zu Chong Zhi Road, Shanghai 201203, China; The CAS Key Laboratory of Receptor Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences (CAS), 555 Zu Chong Zhi Road, Shangh

Bioorg Med Chem ; 26(8): 1896-1908, 2018 05 01.

Article em En | MEDLINE | ID: mdl-29523469

Assuntos

Desenho de Fármacos; Hipoglicemiantes/síntese química; Pirazóis/química; Receptores de Glucagon/antagonistas & inibidores; Regulação Alostérica; Sítios de Ligação; AMP Cíclico/metabolismo; Células HEK293; Humanos; Hipoglicemiantes/metabolismo; Simulação de Acoplamento Molecular; Ligação Proteica; Estrutura Terciária de Proteína; Pirazóis/metabolismo; Receptores de Glucagon/genética; Receptores de Glucagon/metabolismo; Relação Estrutura-Atividade

Palavras-chave

Binding pocket; Docking study; Glucagon receptor antagonist; Pyrazole derivatives

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Texto completo: 1 Coleções: 01-internacional Temas: Geral Base de dados: MEDLINE Assunto principal: Pirazóis / Desenho de Fármacos / Receptores de Glucagon / Hipoglicemiantes Limite: Humans Idioma: En Revista: Bioorg Med Chem Assunto da revista: BIOQUIMICA / QUIMICA Ano de publicação: 2018 Tipo de documento: Article

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