4-hydroxy-2-quinolones. 178*. irreversible chemical modification of chinoxicaine at the position 4 of the quinolone ring

4-hydroxy-2-quinolones. 178*. irreversible chemical modification of chinoxicaine at the position 4 of the quinolone ring
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4-羟基-2-喹诺酮类。

DOI:
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发表时间:
2010
期刊:
影响因子:
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通讯作者:
E. Y. Kovalenko
E. Y. Kovalenko
中科院分区:
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文献类型:
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作者:
I. Ukrainets;A. A. Tkach;V. Kravtsova;V. Mamchur;E. Y. Kovalenko

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在继续研究提高局部麻醉剂Chinoxicaine的药物活性的同时,我们研究了其4-OH基团对生物电子等排片段的不可逆置换。本文合成了一系列4-R-2-氧代-1,2-二氢喹啉-3-羧酸2-(二乙氨基)乙酰胺盐酸盐。给出了所得到的化合物的局部麻醉性质的实验数据,并进行了讨论。
While continuing our investigation in improving the pharmaceutical activities of the local anesthetic Chinoxicaine we have studied the irreversible replacement of its 4-OH group for bioisosteric fragments. For this purpose the synthesis of a series of 4-R-2-oxo-1,2-dihydroquinoline-3-carboxylic acids 2-(diethylamino)ethylamide hydrochlorides has been carried out. The experimental data of the local anesthetic properties of the compounds obtained are given and discussed.