Design, Practical Synthesis, and Biological Evaluation of Novel 6-(Pyrazolylmethyl)-4-quinoline-3-carboxylic Acid Derivatives as HIV-1 Integrase Inhibitors

被引：19

作者：

Hu, Liming ^{[1
]}

Yan, Song ^{[1
]}

Luo, Zaigang ^{[1
,2
]}

Han, Xiao ^{[1
]}

Wang, Yujie ^{[1
]}

Wang, Zhanyang ^{[1
]}

Zeng, Chengchu ^{[1
]}

机构：

[1] Beijing Univ Technol, Coll Life Sci & Bioengn, Beijing 100124, Peoples R China

[2] Anhui Univ Sci Technol, Coll Chem Engn, Huainan 232001, Peoples R China

来源：

MOLECULES | 2012年 / 17卷 / 09期

基金：

北京市自然科学基金;

关键词：

HIV-1; integrase inhibitors; quinolone-3-carboxylic acid derivatives; PHARMACOPHORE;

D O I：

10.3390/molecules170910652

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

A series of novel 6-(pyrazolylmethyl)-4-oxo-4H-quinoline-3-carboxylic acid derivatives bearing different substituents on the N-position of quinoline ring were designed and synthesized as potential HIV-1 integrase (IN) inhibitors, based on the structurally related GS-9137 scaffold. The structures of all new compounds were confirmed by H-1-NMR, C-13-NMR and ESI (or HRMS) spectra. Detailed synthetic protocols and the anti-IN activity studies are also presented.

引用

页码：10652 / 10666

页数：15

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