[桦木酸及其衍生物的酰肼和取代苯甲酰肼的合成与抗病毒活性]

[Synthesis and antiviral activity of hydrazides and substituted benzalhydrazides of betulinic acid and its derivatives].

作者信息

Flekhter O B, Boreko E I, Nigmatullina L R, Pavlova N I, Nikolaeva S N, Savinova O V, Eremin V F, Baltina L A, Galin F Z, Tolstikov G A

机构信息

Institute of Organic Chemistry, Ufa Scientific Center, Russian Academy of Sciences, pr. Oktyabrya 71, Ufa, Bashkortostan, 450054 Russia.

出版信息

Bioorg Khim. 2003 May-Jun;29(3):326-32. doi: 10.1023/a:1023948919315.

DOI:10.1023/a:1023948919315

PMID:12845810

Abstract

New nitrogen-containing derivatives of betulinic and betulonic acids, hydrazides and N'-benzalhydrazides, were synthesized. Their antiviral activities toward of influenza A virus, herpes simplex type I virus, enterovirus ECHO6, and HIV-1 were studied in vitro. Betulinic acid 3-oxime was found to have the highest activity against the influenza virus. Betulonic acid, betulinic acid 4-chlorobenzalhydrazide, betulonic acid 3-oxime benzalhydrazide, and betulinic acid hydrazide inhibited the replication of herpes simplex type I virus. Betulinic acid hydrazide also showed antiviral activity toward HIV-1. All the derivatives of betulinic acid under study displayed a low antiviral activity toward enterovirus ECHO6.

摘要

合成了桦木酸和桦木酮酸的新型含氮衍生物、酰肼和N'-苯甲酰肼。在体外研究了它们对甲型流感病毒、单纯疱疹I型病毒、肠道病毒ECHO6和HIV-1的抗病毒活性。发现桦木酸3-肟对流感病毒具有最高活性。桦木酮酸、桦木酸4-氯苯甲酰肼、桦木酮酸3-肟苯甲酰肼和桦木酸酰肼抑制单纯疱疹I型病毒的复制。桦木酸酰肼对HIV-1也显示出抗病毒活性。所研究的所有桦木酸衍生物对肠道病毒ECHO6均表现出低抗病毒活性。