Characterisation of Plasmodium falciparum aspartic protease inhibition by piperidine derivatives |
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Authors: | Saify Zafar Saied Nisa Mehrun Azhar Kaniz Fizza Azim M Kamran Rasheed Huma Mushtaq Nousheen Arain M Arshad Haider Shazia Khanum Manawar Ahmed Waseem |
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Institution: | H.E.J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi-75270, Pakistan. zssaify@gmail.com |
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Abstract: | Piperidine derivatives are reported to exhibit a variety of pharmacological activities. In this article, synthesis and aspartic protease inhibitory activity of three nitrophenacyl derivatives of N-methyl-4-hydroxy piperidine are reported. Enzyme assays showed that the attachment of a nitro group in the benzene ring plays an important role in the inhibition of plasmepsin-II of Plasmodium falciparum. The compound 1-methyl-1-(4'-nitrophenacyl)-4-hydroxypiperidinium bromide (3), consisting of a nitro group at the para position, was the most active at the concentration of 1.0?μM. The activity of the compounds was evaluated through the observed orientation and diagrammatic representation of nitrophenacyl derivatives of 4-hydroxy piperidine. |
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