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Synthesis and biological evaluation of longanlactone analogues as neurotrophic agents |
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| Authors: | Chada Raji Reddy Amol Gorgile Tukaram Siddique Z Mohammed Uredi Dilipkumar Bathini Nagendra Babu Sumana Chakravarty Dwaipayan Bhattacharya Pranav C Joshi René Grée |
| Institution: | 1. Division of Natural Products Chemistry, CSIR-Indian Institute of Chemical Technology, Hyderabad 500007, India;2. National Institute of Pharmaceutical Education and Research, Hyderabad 500037 India;3. Centre for Chemical Biology, CSIR-Indian Institute of Chemical Technology, Hyderabad 500007, India;4. Institut des Sciences Chimiques de Rennes, CNRS UMR 6226, Avenue du Général Leclerc, 35042 Rennes Cedex, France |
| 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: | Neurotrophic agent Longanlactone Pyrrole alkaloid |
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