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2-吡啶甲醛、4-吡啶甲醛及4-喹啉甲醛腙的合成与生物活性

Synthesis and biological activity of guanylhydrazones of 2- and 4-pyridine and 4-quinoline carboxaldehydes.

作者信息

Foye W O, Almassian B, Eisenberg M S, Maher T J

机构信息

Samuel M. Best Research Laboratory, Massachusetts College of Pharmacy and Allied Health Sciences, Boston 02115.

出版信息

J Pharm Sci. 1990 Jun;79(6):527-30. doi: 10.1002/jps.2600790615.

Abstract

A series of guanylhydrazones derived from 2- and 4-pyridine and 4-quinoline carboxyaldehydes was synthesized from S-methylisothio-semicarbazide hydroiodide using known procedures. The compounds are analogous to anticancer and antiviral thiosemicarbazones, but several of the guanylhydrazones derived from 4-quinoline carboxaldehyde showed no activity against P388 lymphocytic leukemia in mice. Guanylhydrazones derived from all three heterocyclic aldehydes revealed significant blood pressure lowering effects in the rat, however.

摘要

使用已知方法,由氢碘酸S-甲基异硫代氨基脲合成了一系列衍生自2-吡啶、4-吡啶和4-喹啉甲醛的胍腙。这些化合物类似于抗癌和抗病毒的硫代氨基脲,但一些衍生自4-喹啉甲醛的胍腙对小鼠P388淋巴细胞白血病没有活性。然而,衍生自所有三种杂环醛的胍腙在大鼠中显示出显著的降压作用。

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