Design, synthesis and biological evaluation of N<sup>1</sup>-(isoquinolin-5-yl)-N<sup>2</sup>-phenylpyrrolidine-1,2-dicarboxamide derivatives as potent TRPV1 antagonists.

Gao, Mingxiang; Nie, Cunbin; Li, Jinyu; Song, Beibei; Cheng, Xinru; Sun, Erying; Yan, Lin; Qian, Hai

Design, synthesis and biological evaluation of N¹-(isoquinolin-5-yl)-N²-phenylpyrrolidine-1,2-dicarboxamide derivatives as potent TRPV1 antagonists.

Gao, Mingxiang; Nie, Cunbin; Li, Jinyu; Song, Beibei; Cheng, Xinru; Sun, Erying; Yan, Lin; Qian, Hai.

Afiliación

Gao M; Institute for Innovative Drug Design and Evaluation, School of Pharmacy, Henan University, N. Jinming Ave., Kaifeng, Henan 475004, China.
Nie C; Institute for Innovative Drug Design and Evaluation, School of Pharmacy, Henan University, N. Jinming Ave., Kaifeng, Henan 475004, China.
Li J; Institute for Innovative Drug Design and Evaluation, School of Pharmacy, Henan University, N. Jinming Ave., Kaifeng, Henan 475004, China.
Song B; Institute for Innovative Drug Design and Evaluation, School of Pharmacy, Henan University, N. Jinming Ave., Kaifeng, Henan 475004, China.
Cheng X; Institute for Innovative Drug Design and Evaluation, School of Pharmacy, Henan University, N. Jinming Ave., Kaifeng, Henan 475004, China.
Sun E; Institute for Innovative Drug Design and Evaluation, School of Pharmacy, Henan University, N. Jinming Ave., Kaifeng, Henan 475004, China.
Yan L; Institute for Innovative Drug Design and Evaluation, School of Pharmacy, Henan University, N. Jinming Ave., Kaifeng, Henan 475004, China. Electronic address: yanlin0378@163.com.
Qian H; State Key Laboratory of Natural Medicines, Center of Drug Discovery, China Pharmaceutical University, 24 Tongjiaxiang, Nanjing, Jiangsu 210009, China. Electronic address: qianhai24@163.com.

Bioorg Chem ; 82: 100-108, 2019 02.

Article en En | MEDLINE | ID: mdl-30278281

Asunto(s)

Analgésicos/farmacología; Isoquinolinas/farmacología; Pirrolidinas/farmacología; Canales Catiónicos TRPV/antagonistas & inhibidores; Administración Oral; Analgésicos/administración & dosificación; Analgésicos/síntesis química; Analgésicos/farmacocinética; Animales; Temperatura Corporal/efectos de los fármacos; Relación Dosis-Respuesta a Droga; Diseño de Fármacos; Humanos; Isoquinolinas/administración & dosificación; Isoquinolinas/síntesis química; Isoquinolinas/farmacocinética; Masculino; Ratones; Estructura Molecular; Dolor/tratamiento farmacológico; Pirrolidinas/administración & dosificación; Pirrolidinas/síntesis química; Pirrolidinas/farmacocinética; Ratas; Relación Estructura-Actividad

Palabras clave

5-Aminoisoquinoline urea; Analgesic; Hyperthermia; Transient receptor potential vanilloid type 1

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Texto completo: 1 Bases de datos: MEDLINE Asunto principal: Pirrolidinas / Canales Catiónicos TRPV / Analgésicos / Isoquinolinas Límite: Animals / Humans / Male Idioma: En Revista: Bioorg Chem Año: 2019 Tipo del documento: Article País de afiliación: China

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