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Synthesis of new naphthoisoxazole amide derivatives and study of their biological evaluations

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Abstract

A series of naphthoisoxazole amide derivatives 4ah have been synthesized from naphthoisoxazole acetic acid 3. 2-Acetyl-1-naphthol-1 on reaction with pulverized sodium and diethyl carbonate gave 4-hydroxy naphthopyrone 2 which on Posner reaction gave naphthoisoxazole acetic acid 3. The cytotoxic activity study for inhibiting melanoma cell survival was evaluated on a series of melanoma cell lines. The anticonvulsant activity of these compounds has been evaluated in Wistar rats. A compound called 4h has been found to have anticonvulsant activity comparable to that of the standard drug phenytoin.

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Acknowledgments

The authors are thankful to The Head, Department of Chemistry, Faculty of Science, The M. S. University of Baroda for providing laboratory facility. The authors are also thankful to Dr. Gavin P. Robertson and Dr. Gajanan S. Inamdar, Department of Pharmacology, The Pennsylvania State University College of Medicine, Hershey, Pennsylvania, USA for in vitro screening of compounds against melanoma cancer cell lines. One of them, JNS, is thankful to UGC New Delhi (RFSMS) for financial support.

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Correspondence to Shubhangi S. Soman.

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Soman, S.S., Soni, J.N. & Patel, T.B. Synthesis of new naphthoisoxazole amide derivatives and study of their biological evaluations. Med Chem Res 23, 3803–3809 (2014). https://doi.org/10.1007/s00044-014-0961-9

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  • DOI: https://doi.org/10.1007/s00044-014-0961-9

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