4.5 Article

Microwave-assisted efficient synthesis of pyrazole-fibrate derivatives as stimulators of glucose uptake in skeletal muscle cells

Journal

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 34, Issue -, Pages -

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2020.127760

Keywords

Pyrazolo[3,4-d]pyrimidinones; GLUT4myc translocation; Diabetes mellitus

Funding

  1. CSIR-CDRI, Govt. of India
  2. CSIR, New Delhi
  3. UGC, New Delhi
  4. ICMR, New Delhi

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A series of pyrazolo[3,4-d]pyrimidinones containing fibrate side chains were designed and synthesized using molecular hybridization concept. Four compounds showed significant stimulation of glucose uptake in L6 rat skeletal muscle cells. Among them, compound 3q exhibited the highest increase in GLUT4myc translocation.
The design and synthesis of a series of pyrazolo[3,4-d]pyrimidinones containing fibrate side chains have been accomplished by utilizing the concept of molecular hybridization. All the synthesized compounds were evaluated for the glucose uptake stimulatory effect in L6 rat skeletal muscle cells. Four compounds (3f, 3g, 3j and 3q) were found to show significant stimulation of glucose uptake. Further these four compounds have been examined for their Glut4 translocation stimulatory effect in L6-Glut4myc myotubes. Compound 3q was found to exert maximum increase in GLUT4myc translocation.

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