Synthesis of 5,8-dimethoxy-3-hydroxy-4-quinolone, a reported inhibitor of HIV RT, and evidence the original proposed structure was incorrect.

Synthesis of 5,8-dimethoxy-3-hydroxy-4-quinolone, a reported inhibitor of HIV RT, and evidence the original proposed structure was incorrect.
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5,8-二甲氧基-3-羟基-4-喹诺酮(一种报道的 HIV RT 抑制剂)的合成,以及最初提出的结构不正确的证据。

DOI:
10.1016/s0960-894x(99)00046-3
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发表时间:
1999
影响因子:
2.7
通讯作者:
Aytes,SA
Aytes,SA
中科院分区:
医学4区
文献类型:
--
作者:
Zembower,DE;Aytes,SA

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标题化合物是一种半合成的衍生物,据报道是一种非核苷类逆转录酶抑制剂,以2,5-二甲氧基苯胺为原料,分四步合成。合成的材料与文献报道的材料在物理性质和核磁共振氢谱上都有所不同。生物学评价表明,合成的2对HIV-1RT没有活性,这表明先前对半合成衍生物的结构指定是错误的。
An unambiguous total synthesis of the title compound, a semi-synthetic derivative reported to be a non-nucleoside reverse transcriptase inhibitor, was conducted in four steps from 2,5-dimethoxyaniline. The synthetic material differed from that reported in the literature, both in its physical properties and1H NMR spectrum. Biological evaluation indicated that synthetic 2 was inactive against HIV-1 RT, suggesting that the previous structural assignment of the semi-synthetic derivative was incorrect.
1 型人类免疫缺陷病毒逆转录酶与 DNA 的相互作用。
DOI: --
发表时间: 1994
期刊: Biochemistry
影响因子: 2.9
作者:
M. Bakhanashvili;A. Hizi
通讯作者: A. Hizi