Design, practical synthesis, and biological evaluation of novel 6-(pyrazolylmethyl)-4-quinoline-3-carboxylic acid derivatives as HIV-1 integrase inhibitors.

Liming Hu, Song Yan, Zaigang Luo, Xiao Han, Yujie Wang, Zhanyang Wang, Chengchu Zeng

Molecules (Basel, Switzerland) 2012 Sep 06

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A series of novel 6-(pyrazolylmethyl)-4-oxo-4-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.

Citation

Liming Hu, Song Yan, Zaigang Luo, Xiao Han, Yujie Wang, Zhanyang Wang, Chengchu Zeng. Design, practical synthesis, and biological evaluation of novel 6-(pyrazolylmethyl)-4-quinoline-3-carboxylic acid derivatives as HIV-1 integrase inhibitors. Molecules (Basel, Switzerland). 2012 Sep 06;17(9):10652-66