Discovery of 7-alkyloxy- [1,2,4] triazolo[1,5-a] pyrimidine derivatives as selective positive modulators of GABA<sub>A1</sub> and GABA<sub>A4</sub> receptors with potent antiepileptic activity.

Wu, Jun; Hou, Zhipeng; Wang, Yan; Chen, Liping; Lian, Chengxi; Meng, Qingfei; Zhang, Chaoying; Li, Xiufen; Huang, Longjiang; Yu, Haibo

Discovery of 7-alkyloxy- [1,2,4] triazolo[1,5-a] pyrimidine derivatives as selective positive modulators of GABA_A1 and GABA_A4 receptors with potent antiepileptic activity.

Wu, Jun; Hou, Zhipeng; Wang, Yan; Chen, Liping; Lian, Chengxi; Meng, Qingfei; Zhang, Chaoying; Li, Xiufen; Huang, Longjiang; Yu, Haibo.

Afiliação

Wu J; State Key Laboratory of Bioactive Substance and Function of Natural Medicines, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, 1 Xiannongtan Street, Xicheng district, Beijing 100050, China.
Hou Z; College of Chemical Engineering, Qingdao University of Science and Technology, 53 Zhengzhou Road, Qingdao 266042, China.
Wang Y; College of Chemical Engineering, Qingdao University of Science and Technology, 53 Zhengzhou Road, Qingdao 266042, China.
Chen L; College of Chemical Engineering, Qingdao University of Science and Technology, 53 Zhengzhou Road, Qingdao 266042, China.
Lian C; College of Chemical Engineering, Qingdao University of Science and Technology, 53 Zhengzhou Road, Qingdao 266042, China.
Meng Q; College of Chemical Engineering, Qingdao University of Science and Technology, 53 Zhengzhou Road, Qingdao 266042, China.
Zhang C; College of Chemical Engineering, Qingdao University of Science and Technology, 53 Zhengzhou Road, Qingdao 266042, China.
Li X; College of Chemical Engineering, Qingdao University of Science and Technology, 53 Zhengzhou Road, Qingdao 266042, China.
Huang L; College of Chemical Engineering, Qingdao University of Science and Technology, 53 Zhengzhou Road, Qingdao 266042, China; State Key Laboratory of Bioactive Substance and Function of Natural Medicines, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, 1
Yu H; State Key Laboratory of Bioactive Substance and Function of Natural Medicines, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, 1 Xiannongtan Street, Xicheng district, Beijing 100050, China. Electronic address: haiboyu@imm.ac.cn.

Bioorg Chem ; 119: 105565, 2022 02.

Article em En | MEDLINE | ID: mdl-34929519

Assuntos

Anticonvulsivantes/farmacologia; Epilepsia/tratamento farmacológico; Pirimidinas/farmacologia; Receptores de GABA-A/metabolismo; Convulsões/tratamento farmacológico; Triazóis/farmacologia; Animais; Anticonvulsivantes/síntese química; Anticonvulsivantes/química; Células Cultivadas; Relação Dose-Resposta a Droga; Descoberta de Drogas; Eletrochoque; Epilepsia/induzido quimicamente; Epilepsia/metabolismo; Masculino; Camundongos; Camundongos Endogâmicos; Estrutura Molecular; Neurônios/efeitos dos fármacos; Neurônios/metabolismo; Pentilenotetrazol; Pirimidinas/síntese química; Pirimidinas/química; Ratos; Ratos Sprague-Dawley; Convulsões/induzido quimicamente; Convulsões/metabolismo; Relação Estrutura-Atividade; Triazóis/síntese química; Triazóis/química

Palavras-chave

Anticonvulsant; Epilepsy; GABA receptors; PTZ

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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Pirimidinas / Convulsões / Triazóis / Receptores de GABA-A / Epilepsia / Anticonvulsivantes Limite: Animals Idioma: En Revista: Bioorg Chem Ano de publicação: 2022 Tipo de documento: Article País de afiliação: China

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