Journal
MOLECULES
Volume 17, Issue 9, Pages 10652-10666Publisher
MDPI AG
DOI: 10.3390/molecules170910652
Keywords
HIV-1; integrase inhibitors; quinolone-3-carboxylic acid derivatives
Funding
- National Key Basic Research Program of China [2009CB930200]
- Beijing Natural Science Foundation [7102009]
- Platform of Innovation of Science and Technology of Beijing Municipal Education Committee [PXM 2012_014204_00_000152]
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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 H-1-NMR, C-13-NMR and ESI (or HRMS) spectra. Detailed synthetic protocols and the anti-IN activity studies are also presented.
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