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Synthesis and biological evaluation of bis-N2,N2′-(4-hydroxycoumarin-3-yl)ethylidene]-2,3-dihydroxysuccinodihydrazides
- Source :
- Bioorganic & Medicinal Chemistry Letters. 30:126911
- Publication Year :
- 2020
- Publisher :
- Elsevier BV, 2020.
-
Abstract
- A series of N2,N2′-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 (IC50 = 3.5 μM), and anti-T. brucei (32% viability) and anti-mycobacterial (Visual MIC90 = 15.63 μM) activity.
- Subjects :
- biology
010405 organic chemistry
Organic Chemistry
Clinical Biochemistry
Hydrazine
Pharmaceutical Science
Biological activity
01 natural sciences
Biochemistry
Medicinal chemistry
0104 chemical sciences
Integrase
010404 medicinal & biomolecular chemistry
chemistry.chemical_compound
chemistry
4-Hydroxycoumarin
Anti mycobacterial
Drug Discovery
Tartaric acid
Hiv 1 integrase
biology.protein
Molecular Medicine
Molecular Biology
Biological evaluation
Subjects
Details
- ISSN :
- 0960894X
- Volume :
- 30
- Database :
- OpenAIRE
- Journal :
- Bioorganic & Medicinal Chemistry Letters
- Accession number :
- edsair.doi...........a99e3186fc8219365f1cc2981841243c
- Full Text :
- https://doi.org/10.1016/j.bmcl.2019.126911