4-HYDROXY-2-QUINOLONES. 195*. SYNTHESIS OF NOVEL, POTENTIAL ANALGESICS BASED ON 4-(HETARYLMETHYL)AMINO-2-OXO-1,2-DIHYDROQUINOLINE-3-CARBOXYLIC ACIDS

被引：7

作者：

Ukrainets, I. V. ^{[1
]}

Mospanova, E. V. ^{[2
]}

Savchenkova, L. V. ^{[3
]}

Yankovich, S. I. ^{[3
]}

机构：

[1] Natl Pharmaceut Univ, UA-61002 Kharkov, Ukraine

[2] V Dal E Ukrainian Natl Univ, Inst Chem Technol, UA-93003 Rubizhne, Ukraine

[3] Luhansk State Med Univ, UA-91045 Lugansk, Ukraine

来源：

CHEMISTRY OF HETEROCYCLIC COMPOUNDS | 2011年 / 47卷 / 01期

关键词：

4-N-R-2-oxo-1,2-dihydroquinoline-3-carboxylic acids; analgesic activity; bioisosteric replacement; BIOISOSTERIC REPLACEMENTS; DRUG DESIGN; INHIBITORS;

D O I：

10.1007/s10593-011-0721-4

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

From the viewpoint of the method of bioisosteric replacement we have carried out the synthesis of a series of 4-(hetarylmethyl)amino-2-oxo-1,2-dihydroquinoline-3-carboxylic acids. For several examples it has been shown experimentally that the aromatic ring in the benzyl fragment of 4-benzylamino-2-oxo-1,2-dihydroquinoline-3-carboxylic acid can be replaced by an isosteric heterocycle without lowering the analgesic properties.

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页码：67 / 73

页数：7

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