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Synthesis and biological evaluation of bis-N2,N2′-(4-hydroxycoumarin-3-yl)ethylidene]-2,3-dihydroxysuccinodihydrazides

Authors :
Meloddy H. Manyeruke
Digby F. Warner
Michelle Isaacs
Heinrich C. Hoppe
Perry T. Kaye
Rui W. M. Krause
Ronnett Seldon
Thendamudzimu Tshiwawa
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.

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