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Synthesis of tetracyclic oxindoles and evaluation of their α-glucosidase inhibitory and glucose consumption-promoting activity.
Hao, Lei; Ma, Yujiao; Zhao, Lianbo; Zhang, Yinan; Zhang, Xinying; Ma, Ying; Dodd, Robert H; Sun, Hua; Yu, Peng.
Afiliação
  • Hao L; China International Science and Technology Cooperation Base of Food Nutrition/Safety and Medicinal Chemistry, College of Biotechnology, Tianjin University of Science & Technology, Tianjin 300457, China.
  • Ma Y; China International Science and Technology Cooperation Base of Food Nutrition/Safety and Medicinal Chemistry, College of Biotechnology, Tianjin University of Science & Technology, Tianjin 300457, China.
  • Zhao L; China International Science and Technology Cooperation Base of Food Nutrition/Safety and Medicinal Chemistry, College of Biotechnology, Tianjin University of Science & Technology, Tianjin 300457, China.
  • Zhang Y; China International Science and Technology Cooperation Base of Food Nutrition/Safety and Medicinal Chemistry, College of Biotechnology, Tianjin University of Science & Technology, Tianjin 300457, China.
  • Zhang X; China International Science and Technology Cooperation Base of Food Nutrition/Safety and Medicinal Chemistry, College of Biotechnology, Tianjin University of Science & Technology, Tianjin 300457, China.
  • Ma Y; School of Pharmacy, Tianjin Medical University, Tianjin 300070, China.
  • Dodd RH; China International Science and Technology Cooperation Base of Food Nutrition/Safety and Medicinal Chemistry, College of Biotechnology, Tianjin University of Science & Technology, Tianjin 300457, China; Centre de recherche de Gif-sur-Yvette, Institut de Chimie des Substances Naturelles, UPR 2301
  • Sun H; China International Science and Technology Cooperation Base of Food Nutrition/Safety and Medicinal Chemistry, College of Biotechnology, Tianjin University of Science & Technology, Tianjin 300457, China. Electronic address: sunhua@tust.edu.cn.
  • Yu P; China International Science and Technology Cooperation Base of Food Nutrition/Safety and Medicinal Chemistry, College of Biotechnology, Tianjin University of Science & Technology, Tianjin 300457, China. Electronic address: yupeng@tust.edu.cn.
Bioorg Med Chem Lett ; 30(14): 127264, 2020 07 15.
Article em En | MEDLINE | ID: mdl-32527562
ABSTRACT
A series of tetracyclic oxindole derivatives was synthesized by asymmetric 1, 3-dipole reaction in 2-4 steps in 57-86% overall yields. These compounds were evaluated for α-glucosidase inhibitory and glucose consumption-promoting activity in vitro. Compound 4l competitively and reversibly inhibited α-glucosidase (IC50 = 3.64 µM) with activity 14-fold higher than that of acarbose. Docking analysis substantiated these findings. In addition, compound 4l exhibited significant glucose consumption promoting activity at 1 µM.
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Alfa-Glucosidases / Inibidores de Glicosídeo Hidrolases / Oxindóis / Glucose Limite: Humans Idioma: En Ano de publicação: 2020 Tipo de documento: Article
Texto completo
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Alfa-Glucosidases / Inibidores de Glicosídeo Hidrolases / Oxindóis / Glucose Limite: Humans Idioma: En Ano de publicação: 2020 Tipo de documento: Article