Bioorganic & medicinal chemistry letters, 2020-03, Vol.30 (5), p.126911
2020
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Details
- Autor(en) / Beteiligte
- Titel
- Synthesis and biological evaluation of bis-N 2 ,N 2 '-(4-hydroxycoumarin-3-yl)ethylidene]-2,3-dihydroxysuccinodihydrazides
- Ist Teil von
- Bioorganic & medicinal chemistry letters, 2020-03, Vol.30 (5), p.126911
- Ort / Verlag
- England
- Erscheinungsjahr
- 2020
- Quelle
- MEDLINE
- Beschreibungen/Notizen
- A series of N ,N '-bis[4-hydroxycoumarin-3-yl)ethylidene]-2,3-dihydroxysuccino-hydrazides, containing 4-hydroxycoumarin, hydrazine and tartaric acid moieties, have been prepared and examined for possible biological activity. Several of these compounds exhibit promising HIV-1 integrase inhibition (IC = 3.5 μM), and anti-T. brucei (32% viability) and anti-mycobacterial (Visual MIC90 = 15.63 μM) activity.
- Sprache
- Englisch
- Identifikatoren
- eISSN: 1464-3405DOI: 10.1016/j.bmcl.2019.126911Titel-ID: cdi_pubmed_primary_31952962
- Format
- –
- Schlagworte
- Antifungal Agents - chemical synthesis, Antifungal Agents - metabolism, Antifungal Agents - pharmacology, Antitubercular Agents - chemical synthesis, Antitubercular Agents - metabolism, Antitubercular Agents - pharmacology, Catalytic Domain, Coumarins - chemical synthesis, Coumarins - metabolism, Coumarins - pharmacology, HeLa Cells, HIV Integrase - chemistry, HIV Integrase - metabolism, HIV Integrase Inhibitors - chemical synthesis, HIV Integrase Inhibitors - metabolism, HIV Integrase Inhibitors - pharmacology, HIV-1 - enzymology, Humans, Hydrazines - chemical synthesis, Hydrazines - metabolism, Hydrazines - pharmacology, Microbial Sensitivity Tests, Molecular Docking Simulation, Mycobacterium tuberculosis - drug effects, Protein Binding, Trypanocidal Agents - chemical synthesis, Trypanocidal Agents - metabolism, Trypanocidal Agents - pharmacology, Trypanosoma brucei brucei - drug effects