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  3. Synthesis and biological evaluation of longanlactone analogues as neurotrophic agents

Synthesis and biological evaluation of longanlactone analogues as neurotrophic agents

  • Bioorg Med Chem Lett. 2018 Feb 15;28(4):673-676. doi: 10.1016/j.bmcl.2018.01.020.
Chada Raji Reddy 1,  Amol Gorgile Tukaram 2,  Siddique Z Mohammed 3,  Uredi Dilipkumar 3,  Bathini Nagendra Babu 2,  Sumana Chakravarty 4,  Dwaipayan Bhattacharya 5,  Pranav C Joshi 5,  René Grée 6
Affiliations

Affiliations

  • 1 Division of Natural Products Chemistry, CSIR-Indian Institute of Chemical Technology, Hyderabad 500007, India. Electronic address: rajireddy@iict.res.in.
  • 2 National Institute of Pharmaceutical Education and Research, Hyderabad 500037 India.
  • 3 Division of Natural Products Chemistry, CSIR-Indian Institute of Chemical Technology, Hyderabad 500007, India.
  • 4 Centre for Chemical Biology, CSIR-Indian Institute of Chemical Technology, Hyderabad 500007, India. Electronic address: sumanachak@iict.res.in.
  • 5 Centre for Chemical Biology, CSIR-Indian Institute of Chemical Technology, Hyderabad 500007, India.
  • 6 Institut des Sciences Chimiques de Rennes, CNRS UMR 6226, Avenue du Général Leclerc, 35042 Rennes Cedex, France.
PMID: 29402744 DOI: 10.1016/j.bmcl.2018.01.020
Abstract

Longanlactone analogues were synthesized using a route featuring Friedel-Crafts acylation, Sonogashira coupling and 1,3-dipolar cycloaddition reactions. Structure-activity relationships were investigated for neurotrophic activity. Compound 6 was found to have the most potent neurotrophic activity among all the synthesized analogues in Neuro2a cells as evidenced by a battery of in vitro/cell based assays for assessment of neurogenic and potential neurotrophic activity including neurite outgrowth assay and real time PCR for popular markers of augmented neurotrophic activity. Compound 6 might serve as a template for further development of highly effective neurotrophic molecules.

Keywords

Longanlactone; Neurotrophic agent; Pyrrole alkaloid.

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