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    Semi-Synthetic Pyrazoline Derivatives from Polygonum senegalense Chalcones and their Anti-Microbial Activities

    Evans Okemwa Kenanda1, Leonidah Kerubo Omosa2 Corresponding author

    1. 1Department of Chemistry, School of Pure and Applied Sciences, Kisii University, P.O. Box 408-40200 Kisii, Kenya.
    2. 2Department of Chemistry, School of Physical Sciences, University of Nairobi, P.O. Box 30197-00100 Nairobi, Kenya.

    CORRESPONDENCE

    Evans Okemwa Kenanda

    Department of Chemistry, School of Pure and Applied Sciences, Kisii University, P.O. Box 408-40200 Kisii, Kenya.

    ekenanda@kisiiuniversity.ac.ke

    Volume 7, Issue 1 · pp. 53–60 · PUBLISHED · DOI: 10.5530/pc.2017.1.8

    View on Pharmacogn. Commn. original site ↗

    ABSTRACT

    This paper describes the semi-synthesis and anti-microbial activity of novel pyrazoline derivatives of Polygonum senegalense chalcones. The study was carried out on the understanding that heterocycles with pyrazoline ring systems are known to possess a broad spectrum of biological activities. The derivatives were afforded by refluxing mixtures of chalcones and phen- ylhydrazine, hydrazine hydrate, and / or acetic acid in DMSO or ethanol at low temperatures between 40-60°C in an oil-bath. The products were characterized in by 1H-NMR (200 or 400 MHz), 13C-NMR spectroscopy and ESI-HRMS. NMR data was described in detail for each derivative. The compounds 6-15 have been screened for their in vitro anti-bacterial activity against one gram positive bacteria (S. aureus) and anti-fungal activity against five strains C. krusei, C. neoformans, and C. glabrata. They all showed insignificant antimicrobial activities with lower IC50 as compared to positive control, except compound 7 that demonstrated moderate anti- fungal activity with IC50 values ranging between 8.01 - 13.74 µg/mL against C. krusei, C. neoformans and C. glabrata. The compound also showed anti- bacterial activity of IC50 value 7.56µg/mL against S. aureus. Based on these findings, we recommend that compound 7 should undergo further structural modification in order to optimize its anti-microbial activity.

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      Kenanda, E. O., & Omosa, L. K. (). Semi-Synthetic Pyrazoline Derivatives from Polygonum senegalense Chalcones and their Anti-Microbial Activities. Pharmacognosy Communications, 7(1), 53–60. https://doi.org/10.5530/pc.2017.1.8