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

Molecules

Liming Hu¹  Song Yan¹  Zaigang Luo¹  Xiao Han¹  Yujie Wang¹  Zhanyang Wang¹ 

[1] ¹College of Life Science and Bioengineering, Beijing University of Technology, Beijing 100124, China ²College of Chemical Engineering, Anhui University of Science Technology, Huainan 232001, China

关键词: HIV-1;    integrase inhibitors;    quinolone-3-carboxylic acid derivatives;   

DOI  :  10.3390/molecules170910652

来源: mdpi

【 摘 要 】

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.

【 授权许可】

CC BY   
This is an open access article distributed under the Creative Commons Attribution License (CC BY) which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.