Molecules 2012, 17(9), 10652-10666; doi:10.3390/molecules170910652
Article

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

Liming Hu 1,* email, Song Yan 1 , Zaigang Luo 1,2 , Xiao Han 1 , Yujie Wang 1 , Zhanyang Wang 1  and Chengchu Zeng 1
1 College of Life Science and Bioengineering, Beijing University of Technology, Beijing 100124, China 2 College of Chemical Engineering, Anhui University of Science Technology, Huainan 232001, China
* Author to whom correspondence should be addressed.
Received: 6 July 2012; in revised form: 6 August 2012 / Accepted: 24 August 2012 / Published: 6 September 2012
(This article belongs to the Section Medicinal Chemistry)
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Abstract: 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 1H-NMR, 13C-NMR and ESI (or HRMS) spectra. Detailed synthetic protocols and the anti-IN activity studies are also presented.
Keywords: HIV-1; integrase inhibitors; quinolone-3-carboxylic acid derivatives

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MDPI and ACS Style

Hu, L.; Yan, S.; Luo, Z.; Han, X.; Wang, Y.; Wang, Z.; Zeng, C. Design, Practical Synthesis, and Biological Evaluation of Novel 6-(Pyrazolylmethyl)-4-quinoline-3-carboxylic Acid Derivatives as HIV-1 Integrase Inhibitors. Molecules 2012, 17, 10652-10666.

AMA Style

Hu L, Yan S, Luo Z, Han X, Wang Y, Wang Z, Zeng C. Design, Practical Synthesis, and Biological Evaluation of Novel 6-(Pyrazolylmethyl)-4-quinoline-3-carboxylic Acid Derivatives as HIV-1 Integrase Inhibitors. Molecules. 2012; 17(9):10652-10666.

Chicago/Turabian Style

Hu, Liming; Yan, Song; Luo, Zaigang; Han, Xiao; Wang, Yujie; Wang, Zhanyang; Zeng, Chengchu. 2012. "Design, Practical Synthesis, and Biological Evaluation of Novel 6-(Pyrazolylmethyl)-4-quinoline-3-carboxylic Acid Derivatives as HIV-1 Integrase Inhibitors." Molecules 17, no. 9: 10652-10666.

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