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Molecules. 2012 Sep 6;17(9):10652-66. doi: 10.3390/molecules170910652.

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

Author information

1
College of Life Science and Bioengineering, Beijing University of Technology, Beijing 100124, China. huliming@bjut.edu.cn

Abstract

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.

PMID:
22955454
DOI:
10.3390/molecules170910652
[Indexed for MEDLINE]
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