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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

1,* , 1, 1,2, 1, 1, 1 and 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 / Revised: 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 HIV-1; integrase inhibitors; quinolone-3-carboxylic acid derivatives
This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).

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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.

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