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




Design, Practical Synthesis, and Biological Evaluation of Novel 6-Pyrazolylmethyl-4-quinoline-3-carboxylic Acid Derivatives as HIV-1 Integrase Inhibitors - Download this document for free, or read online. Document in PDF available to download.

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





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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





Author: Liming Hu 1,* , Song Yan 1, Zaigang Luo 1,2, Xiao Han 1, Yujie Wang 1, Zhanyang Wang 1 and Chengchu Zeng 1

Source: http://mdpi.com/



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