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Synthesis and biological evaluation of bis-N2,N2'-(4-hydroxycoumarin-3-yl)ethylidene]-2,3-dihydroxysuccinodihydrazides.
Bioorganic & Medicinal Chemistry Letters ( IF 2.5 ) Pub Date : 2019-12-19 , DOI: 10.1016/j.bmcl.2019.126911
Meloddy H Manyeruke 1 , Thendamudzimu Tshiwawa 1 , Heinrich C Hoppe 2 , Michelle Isaacs 3 , Ronnett Seldon 4 , Digby F Warner 5 , Rui W M Krause 6 , Perry T Kaye 6
Affiliation  

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.

中文翻译:

双-N2,N2'-(4-羟基香豆素-3-基)亚乙基] -2,3-二羟基琥珀酰二酰肼的合成及生物学评价。

已制备了一系列含有4-羟基香豆素,肼和酒石酸部分的N2,N2′-双[4-羟基香豆素-3-基)亚乙基] -2,3-二羟基琥珀酰肼,并检查了其可能的生物学活性。这些化合物中的几种表现出有希望的HIV-1整合酶抑制作用(IC50 = 3.5μM)和抗T。Brucei(32%的活力)和抗分枝杆菌(Visual MIC90 = 15.63μM)活性。
更新日期:2019-12-20
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