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Synthesis, biological evaluation, and modeling studies of inhibitors aimed at the malarial proteases plasmepsins I and II by Daniel Muthas; Daniel Nöteberg; Yogesh A. Sabnis; Elizabeth Hamelink; Lotta Vrang; Bertil Samuelsson; Anders Karlén; Anders Hallberg is a Biochemistry, Genetics and Molecular Biology article available to read on EtoBox.

What is Synthesis, biological evaluation, and modeling studies of inhibitors aimed at the malarial proteases plasmepsins I and II about?

The increasing resistance of the malarial parasite to antimalarial drugs is a major contributor to the reemergence of the disease and increases the need for new drug targets. The two aspartic proteases, plasmepsins I and II, from Plasmodium falciparum have recently emerged as potential targets. In an effort to inhibit these hemoglobinases, a series of inhibitors encompassing a basic hydroxyethylamine transition state isostere as a central fragment were prepared. The synthesized compounds were varied in the P1 0 position and exhibited biological activities in the range of 31 to >2000 nM. To try to rationalize the results, molecular docking and 3D-QSAR analysis were used.

Who reads Synthesis, biological evaluation, and modeling studies of inhibitors aimed at the malarial proteases plasmepsins I and II?

It is typically read by researchers, students, and practitioners in Biochemistry, Genetics and Molecular Biology.

Author
Daniel Muthas; Daniel Nöteberg; Yogesh A. Sabnis; Elizabeth Hamelink; Lotta Vrang; Bertil Samuelsson; Anders Karlén; Anders Hallberg
Publisher
Elsevier Science; Elsevier ; Elsevier Ltd.; Elsevier BV (ISSN 0968-0896)
Published
2005
Language
EN
Field
Biochemistry, Genetics and Molecular Biology (Life Sciences)

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