Synthesis and biological evaluation of bis-N2, N2′-(4-hydroxycoumarin-3-yl)ethylidene]-2, 3-dihydroxysuccinodihydrazides. Issue 5 (1st March 2020)

• Record Type: Journal Article
• Authors: Manyeruke, Meloddy H.; Tshiwawa, Thendamudzimu; Hoppe, Heinrich C.; Isaacs, Michelle; Seldon, Ronnett; Warner, Digby F.; Krause, Rui W.M.; Kaye, Perry T.
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 30:Issue 5(2020)
• Publication Date: 2020-03-01
• Subjects: 4-Hydroxycoumarins -- Succinodihydrazides -- Synthesis -- HIV-1 integrase -- Anti-trypanosomal -- Anti-mycobacterial; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2019.126911
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: Abstract: A series of N 2, N 2 ′-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.