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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

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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 which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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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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