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European journal of medicinal chemistry. 2018 Oct 5:158:801-813. doi: 10.1016/j.ejmech.2018.09.018 Q15.92025

One-pot, multi-component synthesis and structure-activity relationships of peptoid-based histone deacetylase (HDAC) inhibitors targeting malaria parasites

基于肽类似物组蛋白去乙酰化酶抑制剂的多成分合成及其抗疟活性研究 翻译改进

Daniela Diedrich  1, Katharina Stenzel  2, Eva Hesping  3, Yevgeniya Antonova-Koch  4, Tamirat Gebru  5, Sandra Duffy  3, Gillian Fisher  3, Andrea Schöler  6, Stephan Meister  4, Thomas Kurz  1, Vicky M Avery  3, Elizabeth A Winzeler  4, Jana Held  5, Katherine T Andrews  7, Finn K Hansen  8

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作者单位

  • 1 Institut für Pharmazeutische und Medizinische Chemie, Heinrich-Heine-Universität Düsseldorf, Universitätsstr. 1, 40225, Düsseldorf, Germany.
  • 2 Institut für Pharmazeutische und Medizinische Chemie, Heinrich-Heine-Universität Düsseldorf, Universitätsstr. 1, 40225, Düsseldorf, Germany; Griffith Institute for Drug Discovery, Griffith University, Don Young Road, Nathan Campus, QLD, 4111, Australia.
  • 3 Griffith Institute for Drug Discovery, Griffith University, Don Young Road, Nathan Campus, QLD, 4111, Australia.
  • 4 Department of Pediatrics, School of Medicine, University of California, San Diego, La Jolla, CA, 92093, United States.
  • 5 Institut für Tropenmedizin, Eberhard Karls Universität Tübingen, Wilhelmstraße 27, 72074, Tübingen, Germany.
  • 6 Pharmaceutical/Medicinal Chemistry, Institute of Pharmacy, Medical Faculty, Leipzig University, Brüderstraße 34, 04103, Leipzig, Germany.
  • 7 Griffith Institute for Drug Discovery, Griffith University, Don Young Road, Nathan Campus, QLD, 4111, Australia. Electronic address: k.andrews@griffith.edu.au.
  • 8 Institut für Pharmazeutische und Medizinische Chemie, Heinrich-Heine-Universität Düsseldorf, Universitätsstr. 1, 40225, Düsseldorf, Germany; Pharmaceutical/Medicinal Chemistry, Institute of Pharmacy, Medical Faculty, Leipzig University, Brüderstraße 34, 04103, Leipzig, Germany. Electronic address: finn.hansen@uni-leipzig.de.

    • DOI: 10.1016/j.ejmech.2018.09.018 PMID: 30245402

    摘要 Ai翻译

    Malaria drug discovery has shifted from a focus on targeting asexual blood stage parasites, to the development of drugs that can also target exo-erythrocytic forms and/or gametocytes in order to prevent malaria and/or parasite transmission. In this work, we aimed to develop parasite-selective histone deacetylase inhibitors (HDACi) with activity against the disease-causing asexual blood stages of Plasmodium malaria parasites as well as with causal prophylac... ...点击完成人机验证后继续浏览
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    期刊名：European journal of medicinal chemistry

    缩写：EUR J MED CHEM

    ISSN：0223-5234

    e-ISSN：1768-3254

    IF/分区：5.9/Q1

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    One-pot, multi-component synthesis and structure-activity relationships of peptoid-based histone deacetylase (HDAC) inhibitors targeting malaria parasites