دورية أكاديمية
Synthesis and anti-parasitic activity of achiral N-benzylated phosphoramidic acid derivatives.
| العنوان: | Synthesis and anti-parasitic activity of achiral N-benzylated phosphoramidic acid derivatives. |
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| المؤلفون: | Adeyemi CM; Department of Chemistry, Rhodes University, Grahamstown 6140, South Africa., Conibear AC; Department of Chemistry, Rhodes University, Grahamstown 6140, South Africa., Mutorwa MK; Department of Chemistry, Rhodes University, Grahamstown 6140, South Africa., Nokalipa IC; Department of Chemistry, Rhodes University, Grahamstown 6140, South Africa., Isaacs M; Centre for Chemico- and Biomedicinal Research, Rhodes University, Grahamstown 6140, South Africa., Mnkandhla D; Centre for Chemico- and Biomedicinal Research, Rhodes University, Grahamstown 6140, South Africa., Hoppe HC; Department of Biochemistry and Microbiolgy, Rhodes University, Grahamstown 6140, South Africa; Centre for Chemico- and Biomedicinal Research, Rhodes University, Grahamstown 6140, South Africa., Lobb KA; Department of Chemistry, Rhodes University, Grahamstown 6140, South Africa; Centre for Chemico- and Biomedicinal Research, Rhodes University, Grahamstown 6140, South Africa., Klein R; Department of Chemistry, Rhodes University, Grahamstown 6140, South Africa; Centre for Chemico- and Biomedicinal Research, Rhodes University, Grahamstown 6140, South Africa., Kaye PT; Department of Chemistry, Rhodes University, Grahamstown 6140, South Africa; Centre for Chemico- and Biomedicinal Research, Rhodes University, Grahamstown 6140, South Africa. Electronic address: p.kaye@ru.ac.za. |
| المصدر: | Bioorganic chemistry [Bioorg Chem] 2020 Aug; Vol. 101, pp. 103947. Date of Electronic Publication: 2020 May 16. |
| نوع المنشور: | Journal Article; Research Support, Non-U.S. Gov't |
| اللغة: | English |
| بيانات الدورية: | Publisher: Elsevier Country of Publication: United States NLM ID: 1303703 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1090-2120 (Electronic) Linking ISSN: 00452068 NLM ISO Abbreviation: Bioorg Chem Subsets: MEDLINE |
| أسماء مطبوعة: | Publication: Amsterdam : Elsevier Original Publication: New York, London, Academic Press. |
| مواضيع طبية MeSH: | Amides/*chemical synthesis , Amides/*pharmacology , Antimalarials/*chemical synthesis , Antimalarials/*pharmacology , Phosphoric Acids/*chemical synthesis , Phosphoric Acids/*pharmacology , Trypanocidal Agents/*chemical synthesis , Trypanocidal Agents/*pharmacology, Amides/chemistry ; Animals ; Antimalarials/chemistry ; Cattle ; Phosphoric Acids/chemistry ; Plasmodium falciparum/drug effects ; Structure-Activity Relationship |
| مستخلص: | Synthetic pathways have been developed to access a series of N-benzylated phosphoramidic acid derivatives as novel, achiral analogues of the established Plasmodium falciparum 1-deoxy-d-xylulose-5-phosphate reductase (PfDXR) enzyme inhibitor, FR900098. Bioassays of the targeted compounds and their synthetic precursors have revealed minimal antimalarial activity but encouraging anti-trypanosomal activity - in one case with an IC Competing Interests: Declaration of Competing Interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper. (Copyright © 2020 Elsevier Inc. All rights reserved.) |
| فهرسة مساهمة: | Keywords: Anti-malarial; Anti-parasitic; Anti-trypanosomal; N-benzylated phosphoramidate; Nagana Trypanosoma brucei |
| المشرفين على المادة: | 0 (Amides) 0 (Antimalarials) 0 (Phosphoric Acids) 0 (Trypanocidal Agents) 9Q189608GB (phosphoramidic acid) |
| تواريخ الأحداث: | Date Created: 20200620 Date Completed: 20210311 Latest Revision: 20210311 |
| رمز التحديث: | 20240829 |
| DOI: | 10.1016/j.bioorg.2020.103947 |
| PMID: | 32559578 |
| قاعدة البيانات: | MEDLINE |
Full Text Finder | تدمد: | 1090-2120 |
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| DOI: | 10.1016/j.bioorg.2020.103947 |