title: Characterisation of Plasmodium falciparum aspartic protease inhibition by piperidine derivatives.
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.
authors: H.E.J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi-75270, Pakistan. zssaify@gmail.com
authors: Zafar Saied
authors: ZS
authors: Saify
authors: Mehrun
authors: M
authors: Nisa
authors: Kaniz Fizza
authors: KF
authors: Azhar
authors: M Kamran
authors: MK
authors: Azim
authors: Huma
authors: H
authors: Rasheed
authors: Nousheen
authors: N
authors: Mushtaq
authors: M Arshad
authors: MA
authors: Arain
authors: Shazia
authors: S
authors: Haider
authors: Manawar
authors: M
authors: Khanum
authors: Waseem
authors: W
authors: Ahmed
mesh_terms: D016282:Aspartic Acid Endopeptidases / Q000037:antagonists & inhibitors*; D057055:Aspartic Acid Proteases / Q000037:antagonists & inhibitors*; D009596:Nitrophenols / Q000737:chemistry; D010880:Piperidines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D010963:Plasmodium falciparum / Q000201:enzymology*; D011485:Protein Binding; D015800:Protozoan Proteins / Q000037:antagonists & inhibitors*
chemical_list: D009596:Nitrophenols; D010880:Piperidines; D015800:Protozoan Proteins; D057055:Aspartic Acid Proteases; D016282:Aspartic Acid Endopeptidases; C100637:plasmepsin II